retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Summary of the compounds and antiepileptic drugs evaluated in the calcium oscillations assay.
    Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 86/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    1) Product Images from "New In Vitro Phenotypic Assay for Epilepsy: Fluorescent Measurement of Synchronized Neuronal Calcium Oscillations"

    Article Title: New In Vitro Phenotypic Assay for Epilepsy: Fluorescent Measurement of Synchronized Neuronal Calcium Oscillations

    Journal: PLoS ONE

    doi: 10.1371/journal.pone.0084755

    Summary of the compounds and antiepileptic drugs evaluated in the calcium oscillations assay.
    Figure Legend Snippet: Summary of the compounds and antiepileptic drugs evaluated in the calcium oscillations assay.

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    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Retigabine’s effect on excitability of cKO PV-INs. A: representative voltage responses to a ramp protocol in CA1 PV-INs from WT and cKO slices before and after bath application of RTG (10 µM). ( B) : summary graphs showing the effect of 10 µM <t>retigabine</t> (RTG) on action potential number (WT, n = 19; cKO, n = 19; ** p < 0.01, Genotype x Treatment interaction: F=9.5, p <0.01 with two-way ANOVA). ( C ) Bath application of RTG in hippocampal slices significantly hyperpolarized the RMP of PV-INs from both WT and cKO mice, but RTG had a smaller effect on RMP from cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01; interaction: p = 0.046 with two-way ANOVA). (D) Bath application of RTG significantly increased the rheobase of PV-INs from both WT and cKO mice, but RTG had less effects on cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01, interaction: p= 0.046 with two-way ANOVA).
    Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    1) Product Images from "Removal of KCNQ2 from Parvalbumin-expressing Interneurons Improves Anti-Seizure Efficacy of Retigabine"

    Article Title: Removal of KCNQ2 from Parvalbumin-expressing Interneurons Improves Anti-Seizure Efficacy of Retigabine

    Journal: bioRxiv

    doi: 10.1101/2020.12.09.417295

    Retigabine’s effect on excitability of cKO PV-INs. A: representative voltage responses to a ramp protocol in CA1 PV-INs from WT and cKO slices before and after bath application of RTG (10 µM). ( B) : summary graphs showing the effect of 10 µM retigabine (RTG) on action potential number (WT, n = 19; cKO, n = 19; ** p < 0.01, Genotype x Treatment interaction: F=9.5, p <0.01 with two-way ANOVA). ( C ) Bath application of RTG in hippocampal slices significantly hyperpolarized the RMP of PV-INs from both WT and cKO mice, but RTG had a smaller effect on RMP from cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01; interaction: p = 0.046 with two-way ANOVA). (D) Bath application of RTG significantly increased the rheobase of PV-INs from both WT and cKO mice, but RTG had less effects on cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01, interaction: p= 0.046 with two-way ANOVA).
    Figure Legend Snippet: Retigabine’s effect on excitability of cKO PV-INs. A: representative voltage responses to a ramp protocol in CA1 PV-INs from WT and cKO slices before and after bath application of RTG (10 µM). ( B) : summary graphs showing the effect of 10 µM retigabine (RTG) on action potential number (WT, n = 19; cKO, n = 19; ** p < 0.01, Genotype x Treatment interaction: F=9.5, p <0.01 with two-way ANOVA). ( C ) Bath application of RTG in hippocampal slices significantly hyperpolarized the RMP of PV-INs from both WT and cKO mice, but RTG had a smaller effect on RMP from cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01; interaction: p = 0.046 with two-way ANOVA). (D) Bath application of RTG significantly increased the rheobase of PV-INs from both WT and cKO mice, but RTG had less effects on cKO mice (WT, n = 19; cKO, n = 18; ** p < 0.01, interaction: p= 0.046 with two-way ANOVA).

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    conditioning paradigm with retigabine  (Alomone Labs)


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    Alomone Labs conditioning paradigm with retigabine
    (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in <t>retigabine-paired</t> chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.
    Conditioning Paradigm With Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    1) Product Images from "Drug targeting to sites of oxidative stress using the Baeyer-Villiger reaction"

    Article Title: Drug targeting to sites of oxidative stress using the Baeyer-Villiger reaction

    Journal: bioRxiv

    doi: 10.1101/2021.09.03.458872

    (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in retigabine-paired chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.
    Figure Legend Snippet: (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in retigabine-paired chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.

    Techniques Used: Expressing

    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Effects of <t>retigabine</t> on the sensory and motor behaviors following oxaliplatin treatment. Oxaliplatin (oxa, 5 mg/kg, ip) was administrated at Day 0. Retigabine (10 mg/kg, ip, daily) was treated at Day –2, Day –1, Day 0, Day 1, and Day 2. The same groups of animals were tested for mechanical and cold behaviors at Day 3, and were tested for heat and motor behaviors at Day 4. (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups). *, P < 0.05; **, P < 0.01; ****, P < 0.0001; two-way repeated measure ANOVA.
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    1) Product Images from "Oxaliplatin Depolarizes the IB4 – Dorsal Root Ganglion Neurons to Drive the Development of Neuropathic Pain Through TRPM8 in Mice"

    Article Title: Oxaliplatin Depolarizes the IB4 – Dorsal Root Ganglion Neurons to Drive the Development of Neuropathic Pain Through TRPM8 in Mice

    Journal: Frontiers in Molecular Neuroscience

    doi: 10.3389/fnmol.2021.690858

    Effects of retigabine on the sensory and motor behaviors following oxaliplatin treatment. Oxaliplatin (oxa, 5 mg/kg, ip) was administrated at Day 0. Retigabine (10 mg/kg, ip, daily) was treated at Day –2, Day –1, Day 0, Day 1, and Day 2. The same groups of animals were tested for mechanical and cold behaviors at Day 3, and were tested for heat and motor behaviors at Day 4. (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups). *, P < 0.05; **, P < 0.01; ****, P < 0.0001; two-way repeated measure ANOVA.
    Figure Legend Snippet: Effects of retigabine on the sensory and motor behaviors following oxaliplatin treatment. Oxaliplatin (oxa, 5 mg/kg, ip) was administrated at Day 0. Retigabine (10 mg/kg, ip, daily) was treated at Day –2, Day –1, Day 0, Day 1, and Day 2. The same groups of animals were tested for mechanical and cold behaviors at Day 3, and were tested for heat and motor behaviors at Day 4. (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups). *, P < 0.05; **, P < 0.01; ****, P < 0.0001; two-way repeated measure ANOVA.

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    Effects of TC-I on the sensory and motor behaviors following oxaliplatin treatment. The administration of oxaliplatin, the schedule for TC-I (10 mg/kg, ip) treatment (same to the Retigabine treatment), the testing schedule for different types of behaviors were described in the Legend of . (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups). **, P < 0.01; ****, P < 0.0001; two-way repeated measure ANOVA.
    Figure Legend Snippet: Effects of TC-I on the sensory and motor behaviors following oxaliplatin treatment. The administration of oxaliplatin, the schedule for TC-I (10 mg/kg, ip) treatment (same to the Retigabine treatment), the testing schedule for different types of behaviors were described in the Legend of . (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups). **, P < 0.01; ****, P < 0.0001; two-way repeated measure ANOVA.

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    Effects of A-967079 on the sensory and motor behaviors following oxaliplatin treatment. The administration of oxaliplatin, the schedule for A-967079 (A-96, 100 mg/kg, po) treatment (same to the Retigabine and TC-I treatment), the testing schedule for different types of behaviors were described in the Legend of . (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups).
    Figure Legend Snippet: Effects of A-967079 on the sensory and motor behaviors following oxaliplatin treatment. The administration of oxaliplatin, the schedule for A-967079 (A-96, 100 mg/kg, po) treatment (same to the Retigabine and TC-I treatment), the testing schedule for different types of behaviors were described in the Legend of . (A) Paw withdrawal threshold to Von-Frey filament; (B) Score of withdrawal response to acetone; (C) Paw withdrawal latency to radiant heat; and (D) Time stayed on rod at different speeds in rotarod tests ( n = 6 for all groups).

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    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    Retigabine, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    retigabine dihydrocloride  (Alomone Labs)


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    Alomone Labs retigabine dihydrocloride
    Coapplication of low concentrations of ARA-S and <t>retigabine</t> limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.
    Retigabine Dihydrocloride, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 91/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    1) Product Images from "Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity"

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    Journal: The Journal of General Physiology

    doi: 10.1085/jgp.202012576

    Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.
    Figure Legend Snippet: Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.

    Techniques Used:

    ARA-S and retigabine activate hK V 7.2/3 through different mechanisms. (a) Representative current traces and corresponding G ( V ) curve of hK V 7.2/3 before and after application of 3 µM retigabine (RTG). Arrowheads in the current families indicate an activating voltage step to −50 mV. Insert of used voltage clamp protocol. Dashed line shows the curve for 3 µM retigabine normalized to G MAX of control. (b) Concentration-response relation for retigabine effect on V 50 . Data shown as mean ± SEM; n = 4–7. Δ V 50:MAX (maximal shift in V 50 ) = −35 mV; EC 50 = 2 µM. (c) Same as in a, but for hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (d) Mean shift in V 50 induced by 3 µM retigabine on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 4 or 5. Statistics denote Student’s t test. (e) Same as in c, but for the effect of 10 µM ARA-S on hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (f) Mean shift in V 50 induced by 10 µM ARA-S on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 5–8. Statistics denote Student’s t test. ns, nonsignificant; WL, tryptophan to leucine mutation.
    Figure Legend Snippet: ARA-S and retigabine activate hK V 7.2/3 through different mechanisms. (a) Representative current traces and corresponding G ( V ) curve of hK V 7.2/3 before and after application of 3 µM retigabine (RTG). Arrowheads in the current families indicate an activating voltage step to −50 mV. Insert of used voltage clamp protocol. Dashed line shows the curve for 3 µM retigabine normalized to G MAX of control. (b) Concentration-response relation for retigabine effect on V 50 . Data shown as mean ± SEM; n = 4–7. Δ V 50:MAX (maximal shift in V 50 ) = −35 mV; EC 50 = 2 µM. (c) Same as in a, but for hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (d) Mean shift in V 50 induced by 3 µM retigabine on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 4 or 5. Statistics denote Student’s t test. (e) Same as in c, but for the effect of 10 µM ARA-S on hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (f) Mean shift in V 50 induced by 10 µM ARA-S on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 5–8. Statistics denote Student’s t test. ns, nonsignificant; WL, tryptophan to leucine mutation.

    Techniques Used: Concentration Assay, Mutagenesis

    ARA-S activates all K V 7 family members but K V 7.4. (a–e) Representative current traces and corresponding G ( V ) curves for hK V 7.1, hK V 7.2, hK V 7.3_A315T, hK V 7.4, and hK V 7.5 before and after application of 10 µM ARA-S. Arrowheads indicate an activating voltage step to −60 mV except for K V 7.1 and K V 7.4, for which the arrowheads indicate an activating voltage step to −50 mV and −30 mV, respectively. Dashed line in the G ( V ) curve shows the curve for 10 µM ARA-S normalized to G MAX of control. (f and g) Mean shift in V 50 (f) and increase in G MAX (g) induced by 10 µM ARA-S. Data shown as mean ± SEM; n = 9–13. The effect of ARA-S on G MAX of hK V 7.1 and hK V 7.5 might be underestimated because of a tendency of decreasing tail currents in the presence of ARA-S at the most positive voltages (e.g., ), the reason for which remains unknown. (h and i) Same as in f and g, but for 3 µM retigabine (RTG). n = 4–5. Dashed lines in f–i denote effect of indicated treatment on hK V 7.2/3.
    Figure Legend Snippet: ARA-S activates all K V 7 family members but K V 7.4. (a–e) Representative current traces and corresponding G ( V ) curves for hK V 7.1, hK V 7.2, hK V 7.3_A315T, hK V 7.4, and hK V 7.5 before and after application of 10 µM ARA-S. Arrowheads indicate an activating voltage step to −60 mV except for K V 7.1 and K V 7.4, for which the arrowheads indicate an activating voltage step to −50 mV and −30 mV, respectively. Dashed line in the G ( V ) curve shows the curve for 10 µM ARA-S normalized to G MAX of control. (f and g) Mean shift in V 50 (f) and increase in G MAX (g) induced by 10 µM ARA-S. Data shown as mean ± SEM; n = 9–13. The effect of ARA-S on G MAX of hK V 7.1 and hK V 7.5 might be underestimated because of a tendency of decreasing tail currents in the presence of ARA-S at the most positive voltages (e.g., ), the reason for which remains unknown. (h and i) Same as in f and g, but for 3 µM retigabine (RTG). n = 4–5. Dashed lines in f–i denote effect of indicated treatment on hK V 7.2/3.

    Techniques Used:

    Coapplication of low concentrations of ARA-S and retigabine improves the activating effect on hK V 7.2/3. (a) Representative current traces and corresponding G ( V ) curves for hK V 7.2/3 before and after coapplication of 1 µM ARA-S and 1 µM retigabine (RTG). Arrowheads indicate an activating voltage step to −60 mV. Insert of used voltage clamp protocols. Dashed line in the G ( V ) curve shows the curve for coapplication of 1 µM ARA-S and 1 µM retigabine normalized to G MAX of control. (b and c) Mean shift in V 50 (b) and increase in G MAX (c) of hK V 7.2/3 induced by indicated treatment. Data shown as mean ± SEM; n = 7–10. (d) Mean hK V 7.2/3 current fold increase at different voltages induced by indicated treatment. Data shown as mean ± SEM; n = 7–10.
    Figure Legend Snippet: Coapplication of low concentrations of ARA-S and retigabine improves the activating effect on hK V 7.2/3. (a) Representative current traces and corresponding G ( V ) curves for hK V 7.2/3 before and after coapplication of 1 µM ARA-S and 1 µM retigabine (RTG). Arrowheads indicate an activating voltage step to −60 mV. Insert of used voltage clamp protocols. Dashed line in the G ( V ) curve shows the curve for coapplication of 1 µM ARA-S and 1 µM retigabine normalized to G MAX of control. (b and c) Mean shift in V 50 (b) and increase in G MAX (c) of hK V 7.2/3 induced by indicated treatment. Data shown as mean ± SEM; n = 7–10. (d) Mean hK V 7.2/3 current fold increase at different voltages induced by indicated treatment. Data shown as mean ± SEM; n = 7–10.

    Techniques Used:

    Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a) Mean shift in V 50 induced by 10 µM ARA-S, 3 µM retigabine (RTG), or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes a shift in V 50 of −20 mV, which was the approximate effect of each treatment on hK V 7.2/3. (b) Mean increase in G MAX induced by 10 µM ARA-S, 3 µM retigabine, or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes an increase in G MAX of 50%, which was the approximate effect of 10 µM ARA-S on hK V 7.2/3.
    Figure Legend Snippet: Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a) Mean shift in V 50 induced by 10 µM ARA-S, 3 µM retigabine (RTG), or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes a shift in V 50 of −20 mV, which was the approximate effect of each treatment on hK V 7.2/3. (b) Mean increase in G MAX induced by 10 µM ARA-S, 3 µM retigabine, or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes an increase in G MAX of 50%, which was the approximate effect of 10 µM ARA-S on hK V 7.2/3.

    Techniques Used:

    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
    PI(4,5)P 2 regulates the action of <t>Retigabine.</t> (A–C) K + -currents were activated with a +40 mV pulses of variable duration in Xenopus oocytes expression K V 7.2/K V 7.3 channels. Subsequently, the currents were deactivated at −90 mV. These recordings were performed in the absence (A) and the presence of 1 µM (blue diamonds, n = 6) and 5 µM of Retigabine (red triangles, n = 7) (C) . (D–F) A two-exponential function was fitted to deactivating currents and the yielded τ 1 , τ 2 and the fractional contribution of the second component (fraction of τ 2 ) were plotted against t PULSE . ( D–F , respectively). (G–I) Semi-logarithmic version of the plot in (D–F) , detailing τ DEACT for t PULSE up to 1 second. For reference, the equivalent values from were plotted as small black square and small red circles. Black arrows in panels (D–I) indicate the range of t PULSE values at which values were statistically different between the recordings in the presence of 1 µM and 5 µM Retigabine.
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    1) Product Images from "Modulation of K V 7 Channel Deactivation by PI(4,5)P 2"

    Article Title: Modulation of K V 7 Channel Deactivation by PI(4,5)P 2

    Journal: Frontiers in Pharmacology

    doi: 10.3389/fphar.2020.00895

    PI(4,5)P 2 regulates the action of Retigabine. (A–C) K + -currents were activated with a +40 mV pulses of variable duration in Xenopus oocytes expression K V 7.2/K V 7.3 channels. Subsequently, the currents were deactivated at −90 mV. These recordings were performed in the absence (A) and the presence of 1 µM (blue diamonds, n = 6) and 5 µM of Retigabine (red triangles, n = 7) (C) . (D–F) A two-exponential function was fitted to deactivating currents and the yielded τ 1 , τ 2 and the fractional contribution of the second component (fraction of τ 2 ) were plotted against t PULSE . ( D–F , respectively). (G–I) Semi-logarithmic version of the plot in (D–F) , detailing τ DEACT for t PULSE up to 1 second. For reference, the equivalent values from were plotted as small black square and small red circles. Black arrows in panels (D–I) indicate the range of t PULSE values at which values were statistically different between the recordings in the presence of 1 µM and 5 µM Retigabine.
    Figure Legend Snippet: PI(4,5)P 2 regulates the action of Retigabine. (A–C) K + -currents were activated with a +40 mV pulses of variable duration in Xenopus oocytes expression K V 7.2/K V 7.3 channels. Subsequently, the currents were deactivated at −90 mV. These recordings were performed in the absence (A) and the presence of 1 µM (blue diamonds, n = 6) and 5 µM of Retigabine (red triangles, n = 7) (C) . (D–F) A two-exponential function was fitted to deactivating currents and the yielded τ 1 , τ 2 and the fractional contribution of the second component (fraction of τ 2 ) were plotted against t PULSE . ( D–F , respectively). (G–I) Semi-logarithmic version of the plot in (D–F) , detailing τ DEACT for t PULSE up to 1 second. For reference, the equivalent values from were plotted as small black square and small red circles. Black arrows in panels (D–I) indicate the range of t PULSE values at which values were statistically different between the recordings in the presence of 1 µM and 5 µM Retigabine.

    Techniques Used: Expressing

    Overall deactivation kinetics as a function of the t PULSE . (A) As before, to consolidate the analysis of the deactivation kinetics, τ DEACT was plotted against the duration of the +40-mV Pulse (t PULSE ) for currents recorded in the presence of 1 μM and 5 μM Retigabine (blue open diamonds and red oepn hexagons, respectively). (B) The values of τ DEACT were significantly different for t PULSE longer than 61 ms. For reference, the equivalent values from were plotted as black solid square and red solid circles. (C, D) Equivalent τ DEACT -t PULSE plots generated from Wortmannin-treated oocytes.
    Figure Legend Snippet: Overall deactivation kinetics as a function of the t PULSE . (A) As before, to consolidate the analysis of the deactivation kinetics, τ DEACT was plotted against the duration of the +40-mV Pulse (t PULSE ) for currents recorded in the presence of 1 μM and 5 μM Retigabine (blue open diamonds and red oepn hexagons, respectively). (B) The values of τ DEACT were significantly different for t PULSE longer than 61 ms. For reference, the equivalent values from were plotted as black solid square and red solid circles. (C, D) Equivalent τ DEACT -t PULSE plots generated from Wortmannin-treated oocytes.

    Techniques Used: Generated

    To determine whether the decrease in the rate of deactivation was a unique property of the heteromeric K V 7.2/K V 7.3 channel. (A, B) K + -current recordings from oocytes expressing K V 7.2 in the absence and presence of 10μM Retigabine (RTG). (C) τ DEACT was plotted as a function of t PULSE for the homomeric K V 7.2. It was found that the slow down of the deactvation kinetics still occurs when K V 7.2 was expressed alone, suggesting that the hysteretic behavior of these K V 7 channels was not a property emerging from heteromerization ( n = 5). (D) τ DEACT -t PULSE plots in C, replotted with a logarithmic t PULSE to highlight the behavior of τ DEACT at short t PULSE values.
    Figure Legend Snippet: To determine whether the decrease in the rate of deactivation was a unique property of the heteromeric K V 7.2/K V 7.3 channel. (A, B) K + -current recordings from oocytes expressing K V 7.2 in the absence and presence of 10μM Retigabine (RTG). (C) τ DEACT was plotted as a function of t PULSE for the homomeric K V 7.2. It was found that the slow down of the deactvation kinetics still occurs when K V 7.2 was expressed alone, suggesting that the hysteretic behavior of these K V 7 channels was not a property emerging from heteromerization ( n = 5). (D) τ DEACT -t PULSE plots in C, replotted with a logarithmic t PULSE to highlight the behavior of τ DEACT at short t PULSE values.

    Techniques Used: Expressing

    retigabine  (Alomone Labs)


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    retigabine  (Alomone Labs)


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    Alomone Labs retigabine
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    Alomone Labs conditioning paradigm with retigabine
    (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in <t>retigabine-paired</t> chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.
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    Alomone Labs retigabine dihydrocloride
    Coapplication of low concentrations of ARA-S and <t>retigabine</t> limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.
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    (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in retigabine-paired chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.

    Journal: bioRxiv

    Article Title: Drug targeting to sites of oxidative stress using the Baeyer-Villiger reaction

    doi: 10.1101/2021.09.03.458872

    Figure Lengend Snippet: (a) Schematic of spared nerve injury and tissues of interest. (b, c) Once neuropathic pain was established on day 7 after SNI, male (n=6) and female (n=6) mice were treated with oral 1c (350 μmol/kg/day), diroximel fumarate (350 μmol/kg/day), or vehicle every day for 3 days (gray box). (b) Mechanical allodynia and (c) dynamic allodynia were assessed. Relative to vehicle: * P <0.05, ** P <0.01, *** P <0.001; 1c vs. diroximel fumarate: ## P <0.01, ### P <0.001. (d) Seven days after SNI, male (n=3) and female (n=3) mice were treated with oral 1c (350 μmol/kg/day) or subcutaneous morphine (3 mg/kg, b.i.d.). Relative to 1c Day 0 (D0, prior to surgery): ** P <0.01, *** P <0.001; relative to morphine D0: # P <0.05, ### P <0.001. (e) Male (n=3) and female (n=3) mice were treated with oral 1c (350 µmol/kg/day), diroximel fumarate (350 µmol/kg/day) or vehicle every day for 7 days, beginning 7 days after SNI or sham surgery. Presence of ongoing pain was interpreted as an increase in time spent in retigabine-paired chamber (conditioning stimulus) after 7 days of treatment, relative to baseline. Relative to sham-vehicle: †† P <0.01; relative to SNI-vehicle: * P <0.05, *** P <0.001. (f) Male and female Nfe2l2 -/- and wildtype control mice (n=3/sex/group) were treated with oral 1c (350 μmol/kg/day), beginning 7 days after SNI, and mechanical allodynia assessed. Relative to wildtype controls: *** P <0.001. (g) L4/5 DRG from 3 mice were pooled after 3 days of treatment, and nuclear extracts were probed for Nrf2 (n=2 males, n=2 females). Relative to ipsilateral vehicle: *** P <0.001; relative to contralateral vehicle and 1c : ††† P <0.001. (h) Antioxidant gene expression L4/5 DRG was determined after 3 days of treatment (n=3 males, n=3 females). Relative to ipsilateral vehicle: * P <0.05, ** P <0.01; relative to contralateral vehicle: # P <0.05; relative to contralateral 1c : † P <0.05; †† P <0.01, ††† P <0.001. ( i ) Naive male (n=3) and female (n = 3) mice were orally treated with 1c (350 µmol/kg), diroximel fumarate (350 µmol/kg), or vehicle daily for 10 days. Blood was collected by cardiac puncture and leukocytes were manually counted. Relative to vehicle: * P <0.05. Individual replicates are presented in spaghetti plots or grey dots.

    Article Snippet: Average scores for each mouse were obtained from three stimulations at intervals of at least 3 min. Spontaneous pain was tested using a conditioning paradigm with retigabine (#R-100; Alomone Laboratory, Jerusalem, Israel) as the conditioned stimulus to briefly relieve pain, as previously described , , .

    Techniques: Expressing

    Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.

    Journal: The Journal of General Physiology

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    doi: 10.1085/jgp.202012576

    Figure Lengend Snippet: Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a and b) Representative current traces and corresponding G ( V ) curves for hK V 7.4 before and after application of either 3 µM retigabine (RTG; a) or coapplication of 1 µM ARA-S and 1 µM retigabine (b). Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. (c) Representative current traces and corresponding G ( V ) curves for hK V 7.1 before and after coapplication of 1 µM ARA-S and 1 µM retigabine. Arrowheads indicate an activating voltage step to −40 mV. Insert of used voltage clamp protocols. Dashed lines in the G ( V ) curves show the curve for each test compound normalized to G MAX of control.

    Article Snippet: Retigabine dihydrocloride was bought from Alomone Labs. N-docosahexaenoyl-L-serine (DOC-S), N-linoleoyl-L-serine (LIN-S), N-arachidonoyl-D-serine, and N-arachidoyl-L-serine (arachidoyl-S) were synthesized in house.

    Techniques:

    ARA-S and retigabine activate hK V 7.2/3 through different mechanisms. (a) Representative current traces and corresponding G ( V ) curve of hK V 7.2/3 before and after application of 3 µM retigabine (RTG). Arrowheads in the current families indicate an activating voltage step to −50 mV. Insert of used voltage clamp protocol. Dashed line shows the curve for 3 µM retigabine normalized to G MAX of control. (b) Concentration-response relation for retigabine effect on V 50 . Data shown as mean ± SEM; n = 4–7. Δ V 50:MAX (maximal shift in V 50 ) = −35 mV; EC 50 = 2 µM. (c) Same as in a, but for hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (d) Mean shift in V 50 induced by 3 µM retigabine on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 4 or 5. Statistics denote Student’s t test. (e) Same as in c, but for the effect of 10 µM ARA-S on hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (f) Mean shift in V 50 induced by 10 µM ARA-S on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 5–8. Statistics denote Student’s t test. ns, nonsignificant; WL, tryptophan to leucine mutation.

    Journal: The Journal of General Physiology

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    doi: 10.1085/jgp.202012576

    Figure Lengend Snippet: ARA-S and retigabine activate hK V 7.2/3 through different mechanisms. (a) Representative current traces and corresponding G ( V ) curve of hK V 7.2/3 before and after application of 3 µM retigabine (RTG). Arrowheads in the current families indicate an activating voltage step to −50 mV. Insert of used voltage clamp protocol. Dashed line shows the curve for 3 µM retigabine normalized to G MAX of control. (b) Concentration-response relation for retigabine effect on V 50 . Data shown as mean ± SEM; n = 4–7. Δ V 50:MAX (maximal shift in V 50 ) = −35 mV; EC 50 = 2 µM. (c) Same as in a, but for hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (d) Mean shift in V 50 induced by 3 µM retigabine on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 4 or 5. Statistics denote Student’s t test. (e) Same as in c, but for the effect of 10 µM ARA-S on hK V 7.2_W236L/hK V 7.3_W265L. Arrowheads indicate an activating voltage step to −60 mV. (f) Mean shift in V 50 induced by 10 µM ARA-S on WT hK V 7.2/3 or hK V 7.2_W236L/hK V 7.3_W265L. Data shown as mean ± SEM; n = 5–8. Statistics denote Student’s t test. ns, nonsignificant; WL, tryptophan to leucine mutation.

    Article Snippet: Retigabine dihydrocloride was bought from Alomone Labs. N-docosahexaenoyl-L-serine (DOC-S), N-linoleoyl-L-serine (LIN-S), N-arachidonoyl-D-serine, and N-arachidoyl-L-serine (arachidoyl-S) were synthesized in house.

    Techniques: Concentration Assay, Mutagenesis

    ARA-S activates all K V 7 family members but K V 7.4. (a–e) Representative current traces and corresponding G ( V ) curves for hK V 7.1, hK V 7.2, hK V 7.3_A315T, hK V 7.4, and hK V 7.5 before and after application of 10 µM ARA-S. Arrowheads indicate an activating voltage step to −60 mV except for K V 7.1 and K V 7.4, for which the arrowheads indicate an activating voltage step to −50 mV and −30 mV, respectively. Dashed line in the G ( V ) curve shows the curve for 10 µM ARA-S normalized to G MAX of control. (f and g) Mean shift in V 50 (f) and increase in G MAX (g) induced by 10 µM ARA-S. Data shown as mean ± SEM; n = 9–13. The effect of ARA-S on G MAX of hK V 7.1 and hK V 7.5 might be underestimated because of a tendency of decreasing tail currents in the presence of ARA-S at the most positive voltages (e.g., ), the reason for which remains unknown. (h and i) Same as in f and g, but for 3 µM retigabine (RTG). n = 4–5. Dashed lines in f–i denote effect of indicated treatment on hK V 7.2/3.

    Journal: The Journal of General Physiology

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    doi: 10.1085/jgp.202012576

    Figure Lengend Snippet: ARA-S activates all K V 7 family members but K V 7.4. (a–e) Representative current traces and corresponding G ( V ) curves for hK V 7.1, hK V 7.2, hK V 7.3_A315T, hK V 7.4, and hK V 7.5 before and after application of 10 µM ARA-S. Arrowheads indicate an activating voltage step to −60 mV except for K V 7.1 and K V 7.4, for which the arrowheads indicate an activating voltage step to −50 mV and −30 mV, respectively. Dashed line in the G ( V ) curve shows the curve for 10 µM ARA-S normalized to G MAX of control. (f and g) Mean shift in V 50 (f) and increase in G MAX (g) induced by 10 µM ARA-S. Data shown as mean ± SEM; n = 9–13. The effect of ARA-S on G MAX of hK V 7.1 and hK V 7.5 might be underestimated because of a tendency of decreasing tail currents in the presence of ARA-S at the most positive voltages (e.g., ), the reason for which remains unknown. (h and i) Same as in f and g, but for 3 µM retigabine (RTG). n = 4–5. Dashed lines in f–i denote effect of indicated treatment on hK V 7.2/3.

    Article Snippet: Retigabine dihydrocloride was bought from Alomone Labs. N-docosahexaenoyl-L-serine (DOC-S), N-linoleoyl-L-serine (LIN-S), N-arachidonoyl-D-serine, and N-arachidoyl-L-serine (arachidoyl-S) were synthesized in house.

    Techniques:

    Coapplication of low concentrations of ARA-S and retigabine improves the activating effect on hK V 7.2/3. (a) Representative current traces and corresponding G ( V ) curves for hK V 7.2/3 before and after coapplication of 1 µM ARA-S and 1 µM retigabine (RTG). Arrowheads indicate an activating voltage step to −60 mV. Insert of used voltage clamp protocols. Dashed line in the G ( V ) curve shows the curve for coapplication of 1 µM ARA-S and 1 µM retigabine normalized to G MAX of control. (b and c) Mean shift in V 50 (b) and increase in G MAX (c) of hK V 7.2/3 induced by indicated treatment. Data shown as mean ± SEM; n = 7–10. (d) Mean hK V 7.2/3 current fold increase at different voltages induced by indicated treatment. Data shown as mean ± SEM; n = 7–10.

    Journal: The Journal of General Physiology

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    doi: 10.1085/jgp.202012576

    Figure Lengend Snippet: Coapplication of low concentrations of ARA-S and retigabine improves the activating effect on hK V 7.2/3. (a) Representative current traces and corresponding G ( V ) curves for hK V 7.2/3 before and after coapplication of 1 µM ARA-S and 1 µM retigabine (RTG). Arrowheads indicate an activating voltage step to −60 mV. Insert of used voltage clamp protocols. Dashed line in the G ( V ) curve shows the curve for coapplication of 1 µM ARA-S and 1 µM retigabine normalized to G MAX of control. (b and c) Mean shift in V 50 (b) and increase in G MAX (c) of hK V 7.2/3 induced by indicated treatment. Data shown as mean ± SEM; n = 7–10. (d) Mean hK V 7.2/3 current fold increase at different voltages induced by indicated treatment. Data shown as mean ± SEM; n = 7–10.

    Article Snippet: Retigabine dihydrocloride was bought from Alomone Labs. N-docosahexaenoyl-L-serine (DOC-S), N-linoleoyl-L-serine (LIN-S), N-arachidonoyl-D-serine, and N-arachidoyl-L-serine (arachidoyl-S) were synthesized in house.

    Techniques:

    Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a) Mean shift in V 50 induced by 10 µM ARA-S, 3 µM retigabine (RTG), or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes a shift in V 50 of −20 mV, which was the approximate effect of each treatment on hK V 7.2/3. (b) Mean increase in G MAX induced by 10 µM ARA-S, 3 µM retigabine, or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes an increase in G MAX of 50%, which was the approximate effect of 10 µM ARA-S on hK V 7.2/3.

    Journal: The Journal of General Physiology

    Article Title: Combining endocannabinoids with retigabine for enhanced M-channel effect and improved K V 7 subtype selectivity

    doi: 10.1085/jgp.202012576

    Figure Lengend Snippet: Coapplication of low concentrations of ARA-S and retigabine limits the off-target effect on other hK V 7 subtypes. (a) Mean shift in V 50 induced by 10 µM ARA-S, 3 µM retigabine (RTG), or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes a shift in V 50 of −20 mV, which was the approximate effect of each treatment on hK V 7.2/3. (b) Mean increase in G MAX induced by 10 µM ARA-S, 3 µM retigabine, or 1 µM ARA-S + 1 µM retigabine coapplied on indicated channels. Data shown as mean ± SEM; n = 4–13. Dashed line denotes an increase in G MAX of 50%, which was the approximate effect of 10 µM ARA-S on hK V 7.2/3.

    Article Snippet: Retigabine dihydrocloride was bought from Alomone Labs. N-docosahexaenoyl-L-serine (DOC-S), N-linoleoyl-L-serine (LIN-S), N-arachidonoyl-D-serine, and N-arachidoyl-L-serine (arachidoyl-S) were synthesized in house.

    Techniques: