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  • 99
    Millipore damgo
    Damgo, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 385 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    94
    Tocris damgo
    Spinal μ-opioid receptor <t>(MOR)</t> activation reduces nociceptive responses in all ages. (A) Typical electromyographic (EMG) traces in postnatal day (P)10, P21, and adult rats during baseline (without any stimulation), predrug (a typical threshold response before application of drug) and postdrug (A: <t>DAMGO</t> 30 ng; B: CTOP 120 ng) periods. The application of MOR opioid agonist DAMGO onto the spinal cord produced antinociceptive responses in all ages tested. Spinal reflex excitability (C) was decreased when compared to age-matched saline and predrug responses in all ages, both saline and CTOP had no significant effect. Mechanical threshold (D) was increased when DAMGO was administered in P10 and P21 rats. ++ , ++++ P
    Damgo, supplied by Tocris, used in various techniques. Bioz Stars score: 94/100, based on 217 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    92
    Bachem damgo
    Relative efficacy values for <t>DAMGO,</t> <t>etorphine,</t> endomorphin-2, and morphine for five MOPr signaling outputs. Values refer to efficacy relative to that of DAMGO, which was set to 1.00 for each output. The values for [ 35 S]GTPγS binding and arrestin-3
    Damgo, supplied by Bachem, used in various techniques. Bioz Stars score: 92/100, based on 72 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    damgo  (Abcam)
    90
    Abcam damgo
    Modeling mu opioid receptor modulation in EMLO-derived neuronal cultures. a , TUJ1/OPRM1 IF in day 22 H3.3.1 EMLO. High magnification images provided (bottom-left) with multi-dimensional view of gut tube (bottom-right). b , Top: OPRM1 expression in apical aspect of neural rosettes and basal neurons. Bottom: TFAP2α expression at the basal aspect of GABAergic rosettes. c , Fluo-4 AM in dissociated EMLO cultures. High magnification image with example soma ROI (right). d , 2D adherent spinal sensory neurons (top, TUJ1/BRN3A) and spinal motor neurons (bottom, TUJ1/Nkx-6.1) used as controls for opioid-responsive firing. e , Examples of calcium transients quantified in dissociated EMLO neuronal soma using Fluo-4 AM. Shown are no calcium transients (none), one transient (single), or multiple transients (multiple) within a 1.5 min acquisition window. f , Histogram of percent of neurons with multiple calcium transients. EMLO dissociated cultures were compared to spinal sensory neurons (positive control) and spinal motor neurons (negative control). Baseline firing in <t>BrainPhys</t> was compared to addition of 1 μM <t>DAMGO,</t> followed by 10 μM Naloxone in the same cultures. n = number of neurons quantified. Individual scale bars provided. Data reported as (mean ±s.e.m.).
    Damgo, supplied by Abcam, used in various techniques. Bioz Stars score: 90/100, based on 7 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    92
    Peninsula Laboratories damgo
    Modeling mu opioid receptor modulation in EMLO-derived neuronal cultures. a , TUJ1/OPRM1 IF in day 22 H3.3.1 EMLO. High magnification images provided (bottom-left) with multi-dimensional view of gut tube (bottom-right). b , Top: OPRM1 expression in apical aspect of neural rosettes and basal neurons. Bottom: TFAP2α expression at the basal aspect of GABAergic rosettes. c , Fluo-4 AM in dissociated EMLO cultures. High magnification image with example soma ROI (right). d , 2D adherent spinal sensory neurons (top, TUJ1/BRN3A) and spinal motor neurons (bottom, TUJ1/Nkx-6.1) used as controls for opioid-responsive firing. e , Examples of calcium transients quantified in dissociated EMLO neuronal soma using Fluo-4 AM. Shown are no calcium transients (none), one transient (single), or multiple transients (multiple) within a 1.5 min acquisition window. f , Histogram of percent of neurons with multiple calcium transients. EMLO dissociated cultures were compared to spinal sensory neurons (positive control) and spinal motor neurons (negative control). Baseline firing in <t>BrainPhys</t> was compared to addition of 1 μM <t>DAMGO,</t> followed by 10 μM Naloxone in the same cultures. n = number of neurons quantified. Individual scale bars provided. Data reported as (mean ±s.e.m.).
    Damgo, supplied by Peninsula Laboratories, used in various techniques. Bioz Stars score: 92/100, based on 11 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    93
    Millipore trifluoroacetate salt
    Modeling mu opioid receptor modulation in EMLO-derived neuronal cultures. a , TUJ1/OPRM1 IF in day 22 H3.3.1 EMLO. High magnification images provided (bottom-left) with multi-dimensional view of gut tube (bottom-right). b , Top: OPRM1 expression in apical aspect of neural rosettes and basal neurons. Bottom: TFAP2α expression at the basal aspect of GABAergic rosettes. c , Fluo-4 AM in dissociated EMLO cultures. High magnification image with example soma ROI (right). d , 2D adherent spinal sensory neurons (top, TUJ1/BRN3A) and spinal motor neurons (bottom, TUJ1/Nkx-6.1) used as controls for opioid-responsive firing. e , Examples of calcium transients quantified in dissociated EMLO neuronal soma using Fluo-4 AM. Shown are no calcium transients (none), one transient (single), or multiple transients (multiple) within a 1.5 min acquisition window. f , Histogram of percent of neurons with multiple calcium transients. EMLO dissociated cultures were compared to spinal sensory neurons (positive control) and spinal motor neurons (negative control). Baseline firing in <t>BrainPhys</t> was compared to addition of 1 μM <t>DAMGO,</t> followed by 10 μM Naloxone in the same cultures. n = number of neurons quantified. Individual scale bars provided. Data reported as (mean ±s.e.m.).
    Trifluoroacetate Salt, supplied by Millipore, used in various techniques. Bioz Stars score: 93/100, based on 9 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    92
    Phoenix Pharmaceuticals damgo
    <t>Endothelin</t> effects on channel mutants A , diagrams depict channel mutants: Kir3.4 (S143T) parent, N-terminal truncation, and chimeras. We produced the Kir3.4(S143T) using a cDNA template for cRNA coding a Kir3.4(S143T) having a truncated (1–57) N terminus. We used Kir3 chimeras: Kir3.4(S143T)-(1–338)/Kir3.1-(333–501) and Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). B , oocytes were injected with 1 ng of MOR and 1 ng of HETAR, and either 1 ng of Kir3.4(S143T), 1 ng of Kir3.4(S143T)-(Δ1–57), 1 ng of Kir3.4(S143T)-(1–338)/Kir3.1-(333–501), or 1 ng of Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). The percent inhibition of the second mu opioid response after Et-1 pretreatment is shown. The bar graph summarizes the effects of Et-1 on the <t>DAMGO</t> activation of MOR compared with untreated controls from the same batch. Data are means ± S.E. from four to seven oocytes and two to three independent experiments.
    Damgo, supplied by Phoenix Pharmaceuticals, used in various techniques. Bioz Stars score: 92/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore d ala2 n me phe4 gly5 ol enkephalin acetate salt
    Unilateral dialysis during the day of <t>100μM</t> <t>DAMGO</t> (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.
    D Ala2 N Me Phe4 Gly5 Ol Enkephalin Acetate Salt, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 5 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    92
    Hello Bio Inc damgo
    Unilateral dialysis during the day of <t>100μM</t> <t>DAMGO</t> (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.
    Damgo, supplied by Hello Bio Inc, used in various techniques. Bioz Stars score: 92/100, based on 6 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    89
    American Radiolabeled Chemicals Inc h damgo
    Unilateral dialysis during the day of <t>100μM</t> <t>DAMGO</t> (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.
    H Damgo, supplied by American Radiolabeled Chemicals Inc, used in various techniques. Bioz Stars score: 89/100, based on 5 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    90
    PolyPeptide Laboratories h damgo
    Unilateral dialysis during the day of <t>100μM</t> <t>DAMGO</t> (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.
    H Damgo, supplied by PolyPeptide Laboratories, used in various techniques. Bioz Stars score: 90/100, based on 5 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    PerkinElmer net902250uc
    Unilateral dialysis during the day of <t>100μM</t> <t>DAMGO</t> (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.
    Net902250uc, supplied by PerkinElmer, used in various techniques. Bioz Stars score: 99/100, based on 12 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    90
    Merck & Co damgo acetate salt
    Membrane potential regulates μ receptor‐induced K ir 3.X currents in <t>HEK293T</t> cells. (a) Representative recording (out of n = 6) of inward K + currents in HEK293T cells expressing wild‐type μ receptors (MOP‐wt) and K ir 3.X channels is shown. K ir 3.X currents were evoked by 4.5 nM morphine (Mor) and 30 nM <t>DAMGO</t> and measured at −90 and −20 mV (voltage protocol is depicted at the bottom; note that depolarization to −20 mV shifts both basal and active currents due to the current–voltage relationship [see Figure S1 ] of the channel). Levels that were used for calculation of maximum responses are shown as light grey line (−90 mV) or dark grey line (−20 mV), and amplitude height is shown by boxes (morphine response: filled box; maximum DAMGO response: empty box). (b) K ir 3.X current responses evoked by non‐saturating morphine concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 6, for further explanation of evaluation, see Section 2 ). (c) Representative recording (out of n = 7) of inward K + currents. K ir 3.X currents were evoked by 3 nM morphine and 30 nM DAMGO and measured and evaluated as explained in (a) (non‐saturating DAMGO response: filled box; saturating response: empty box). (d) K ir 3.X current responses evoked by non‐saturating DAMGO concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 7, for further explanation of evaluation, see Section 2 ). Responses at −90 and −20 mV were compared in the same recording. * P
    Damgo Acetate Salt, supplied by Merck & Co, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    99
    Millipore damgo acetate
    <t>DAMGO-induced</t> activation of [ 35 S]- <t>GTPγS</t> binding in P450-deficient and control mouse brains. A) Membranes prepared from control (WT) and Null whole brains were incubated with [ 35 S]-GTPγS and the specified concentrations of DAMGO (abscissa, log M), then filtered as described. Specifically bound [ 35 S]- GTPγS values (ordinate, % of basal binding, mean ± S.E.M.) are shown for 3 male subjects from each genotype. Basal binding (in the absence of DAMGO) was 204.4 ± 34.4 and 180.8 ± 4.6 fmol/mg protein (mean ± S.E.M.) for WT and Null , respectively, not significantly different from each other. B) [ 35 S]-GTPγS binding values are shown (as in A) for membranes incubated with DAMGO (10 µM) for seven specified CNS regions from five male subjects of each genotype. Basal binding values (mean ± S.E.M.) ranged from 87.9 ± 10.3 and 64.5 ± 9.9 (WT, Null , respectively for spinal cord) to 215.9 ± 16.0 and 228.0 ± 60.0 (WT, Null , respectively for neocortex). ANOVA of basal binding values found significant (P
    Damgo Acetate, supplied by Millipore, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    86
    Pro-Lab damgo injection increased total daily intake
    <t>DAMGO-induced</t> activation of [ 35 S]- <t>GTPγS</t> binding in P450-deficient and control mouse brains. A) Membranes prepared from control (WT) and Null whole brains were incubated with [ 35 S]-GTPγS and the specified concentrations of DAMGO (abscissa, log M), then filtered as described. Specifically bound [ 35 S]- GTPγS values (ordinate, % of basal binding, mean ± S.E.M.) are shown for 3 male subjects from each genotype. Basal binding (in the absence of DAMGO) was 204.4 ± 34.4 and 180.8 ± 4.6 fmol/mg protein (mean ± S.E.M.) for WT and Null , respectively, not significantly different from each other. B) [ 35 S]-GTPγS binding values are shown (as in A) for membranes incubated with DAMGO (10 µM) for seven specified CNS regions from five male subjects of each genotype. Basal binding values (mean ± S.E.M.) ranged from 87.9 ± 10.3 and 64.5 ± 9.9 (WT, Null , respectively for spinal cord) to 215.9 ± 16.0 and 228.0 ± 60.0 (WT, Null , respectively for neocortex). ANOVA of basal binding values found significant (P
    Damgo Injection Increased Total Daily Intake, supplied by Pro-Lab, used in various techniques. Bioz Stars score: 86/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Bachem damgo tyr d ala gly nme phe gly ol
    <t>DAMGO-induced</t> activation of [ 35 S]- <t>GTPγS</t> binding in P450-deficient and control mouse brains. A) Membranes prepared from control (WT) and Null whole brains were incubated with [ 35 S]-GTPγS and the specified concentrations of DAMGO (abscissa, log M), then filtered as described. Specifically bound [ 35 S]- GTPγS values (ordinate, % of basal binding, mean ± S.E.M.) are shown for 3 male subjects from each genotype. Basal binding (in the absence of DAMGO) was 204.4 ± 34.4 and 180.8 ± 4.6 fmol/mg protein (mean ± S.E.M.) for WT and Null , respectively, not significantly different from each other. B) [ 35 S]-GTPγS binding values are shown (as in A) for membranes incubated with DAMGO (10 µM) for seven specified CNS regions from five male subjects of each genotype. Basal binding values (mean ± S.E.M.) ranged from 87.9 ± 10.3 and 64.5 ± 9.9 (WT, Null , respectively for spinal cord) to 215.9 ± 16.0 and 228.0 ± 60.0 (WT, Null , respectively for neocortex). ANOVA of basal binding values found significant (P
    Damgo Tyr D Ala Gly Nme Phe Gly Ol, supplied by Bachem, used in various techniques. Bioz Stars score: 85/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    N/A
    DAMGO is a selective peptide agonist of the µ opioid receptor Ks 1 18 1 430 and 213 nM for human µ δ and κ opioid receptors respectively DAMGO displays
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    N/A
    Synthetic peptice μOR agonist
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    N/A
    DAMGO is a highly selective peptide agonist for the μ opioid receptor Sequence YAGFG Modifications Ala 2 D Ala Phe 4 N methyl Phe Gly 5 Gly ol
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    Image Search Results


    Spinal μ-opioid receptor (MOR) activation reduces nociceptive responses in all ages. (A) Typical electromyographic (EMG) traces in postnatal day (P)10, P21, and adult rats during baseline (without any stimulation), predrug (a typical threshold response before application of drug) and postdrug (A: DAMGO 30 ng; B: CTOP 120 ng) periods. The application of MOR opioid agonist DAMGO onto the spinal cord produced antinociceptive responses in all ages tested. Spinal reflex excitability (C) was decreased when compared to age-matched saline and predrug responses in all ages, both saline and CTOP had no significant effect. Mechanical threshold (D) was increased when DAMGO was administered in P10 and P21 rats. ++ , ++++ P

    Journal: Pain

    Article Title: Postnatal maturation of endogenous opioid systems within the periaqueductal grey and spinal dorsal horn of the rat

    doi: 10.1016/j.pain.2013.09.022

    Figure Lengend Snippet: Spinal μ-opioid receptor (MOR) activation reduces nociceptive responses in all ages. (A) Typical electromyographic (EMG) traces in postnatal day (P)10, P21, and adult rats during baseline (without any stimulation), predrug (a typical threshold response before application of drug) and postdrug (A: DAMGO 30 ng; B: CTOP 120 ng) periods. The application of MOR opioid agonist DAMGO onto the spinal cord produced antinociceptive responses in all ages tested. Spinal reflex excitability (C) was decreased when compared to age-matched saline and predrug responses in all ages, both saline and CTOP had no significant effect. Mechanical threshold (D) was increased when DAMGO was administered in P10 and P21 rats. ++ , ++++ P

    Article Snippet: Drugs DAMGO (MOR-agonist, 30 ng; Tocris, Abingdon, Oxon, UK) and CTOP (MOR-antagonist, 100 ng; Tocris) were administered at doses determined from previously published studies in adult brainstem .

    Techniques: Activation Assay, Produced

    Recruitment of β-arrestin2 by activation of μ-opioid receptors. Stably transfected HEK293 cells coexpressing μ-opioid receptors and β-arrestin2 were pretreated for 60 min with DAMGO or PnPP-19 at the indicated concentrations. The group “DAMGO + PnPP-19” represents prior incubation of the cells with 10 μM of PnPP-19 for 30 min. β-arrestin2 recruitment was quantified by high content imaging complementation assay as described in Materials and Methods ( n = 5).

    Journal: Toxins

    Article Title: The Peptide PnPP-19, a Spider Toxin Derivative, Activates μ-Opioid Receptors and Modulates Calcium Channels

    doi: 10.3390/toxins10010043

    Figure Lengend Snippet: Recruitment of β-arrestin2 by activation of μ-opioid receptors. Stably transfected HEK293 cells coexpressing μ-opioid receptors and β-arrestin2 were pretreated for 60 min with DAMGO or PnPP-19 at the indicated concentrations. The group “DAMGO + PnPP-19” represents prior incubation of the cells with 10 μM of PnPP-19 for 30 min. β-arrestin2 recruitment was quantified by high content imaging complementation assay as described in Materials and Methods ( n = 5).

    Article Snippet: Plates were kept in a humidified incubator at 37 °C filled with 5% CO2 for 24 h. HEK293T were stimulated with the selective opioid agonist DAMGO (Tocris, Minneapolis, MN, USA) or the synthetic peptide PnPP-19 in HEPES-buffered saline solution (HBSS) including 0.1% v / v BSA (10−10 M–10−4 M) for 60 min at 37 °C.

    Techniques: Activation Assay, Stable Transfection, Transfection, Incubation, Imaging

    Relative efficacy values for DAMGO, etorphine, endomorphin-2, and morphine for five MOPr signaling outputs. Values refer to efficacy relative to that of DAMGO, which was set to 1.00 for each output. The values for [ 35 S]GTPγS binding and arrestin-3

    Journal: Molecular Pharmacology

    Article Title: Endomorphin-2: A Biased Agonist at the ?-Opioid Receptor

    doi: 10.1124/mol.112.078659

    Figure Lengend Snippet: Relative efficacy values for DAMGO, etorphine, endomorphin-2, and morphine for five MOPr signaling outputs. Values refer to efficacy relative to that of DAMGO, which was set to 1.00 for each output. The values for [ 35 S]GTPγS binding and arrestin-3

    Article Snippet: Morphine hydrochloride was obtained from Mcfarlan Smith (Edinburgh, UK), etorphine from Research Triangle Institute (Research Triangle Park, NC), and DAMGO from Bachem (Bubendorf, Switzerland).

    Techniques: Binding Assay

    Concentration-response curves for activation of the GIRK current in rat LC neurons by DAMGO, etorphine, and endomorphin-2. In individual LC neurons, concentration-response curves for DAMGO ( n = 3–5) (A), etorphine ( n = 3–8) (B),and endomorphin-2

    Journal: Molecular Pharmacology

    Article Title: Endomorphin-2: A Biased Agonist at the ?-Opioid Receptor

    doi: 10.1124/mol.112.078659

    Figure Lengend Snippet: Concentration-response curves for activation of the GIRK current in rat LC neurons by DAMGO, etorphine, and endomorphin-2. In individual LC neurons, concentration-response curves for DAMGO ( n = 3–5) (A), etorphine ( n = 3–8) (B),and endomorphin-2

    Article Snippet: Morphine hydrochloride was obtained from Mcfarlan Smith (Edinburgh, UK), etorphine from Research Triangle Institute (Research Triangle Park, NC), and DAMGO from Bachem (Bubendorf, Switzerland).

    Techniques: Concentration Assay, Activation Assay

    Anterior insular MORs are necessary to induce mOP-LTD in the DLS. a Schematic figure of coronal brain slice showing the recording of EPSCs evoked by focal electric stimulation in the DLS of MOR-flox mice. An AAV vector encoding for cre-recombinase (AAV.hSyn.cre) was injected 8 weeks prior to recordings. Coronal brain slice showing the infection of anterior insular cortex and dorsal striatal terminal expression (bar scale = 1000 μm). b Representative electrically evoked synaptic traces and a recording time course from the DLS before and after DAMGO (0.3 μM, 5 min) showing the loss of mOP-LTD mediated by anterior insular MORs ( P = 0.136, t 5 = 1.775, n = 6 from 4 mice). c , d Representative electrically evoked synaptic traces and a recording time course from the DLS before and after DAMGO (0.3 μM, 5 min) and high-frequency stimulation (HFS) coupled with depolarization (4 pulses of 100 Hz, 10 s inter-pulse interval). DAMGO application was incapable of producing mOP-LTD in the DLS of anterior insula MOR knockout mice. However, HFS induced a strong reduction of eEPSCs in the DLS, indicating intact eCB-LTD (baseline vs DAMGO: P = 0.262, t 3 = 1.3.78; baseline vs HFS: P = 0.0082, t 3 = 6.259; DAMGO vs HFS: P = 0.0467, t 3 = 3.273; n = 4 from 3 mice). Data analyzed with Student’s paired t tests. Data represent mean ± SEM

    Journal: Nature Communications

    Article Title: Alcohol exposure disrupts mu opioid receptor-mediated long-term depression at insular cortex inputs to dorsolateral striatum

    doi: 10.1038/s41467-018-03683-1

    Figure Lengend Snippet: Anterior insular MORs are necessary to induce mOP-LTD in the DLS. a Schematic figure of coronal brain slice showing the recording of EPSCs evoked by focal electric stimulation in the DLS of MOR-flox mice. An AAV vector encoding for cre-recombinase (AAV.hSyn.cre) was injected 8 weeks prior to recordings. Coronal brain slice showing the infection of anterior insular cortex and dorsal striatal terminal expression (bar scale = 1000 μm). b Representative electrically evoked synaptic traces and a recording time course from the DLS before and after DAMGO (0.3 μM, 5 min) showing the loss of mOP-LTD mediated by anterior insular MORs ( P = 0.136, t 5 = 1.775, n = 6 from 4 mice). c , d Representative electrically evoked synaptic traces and a recording time course from the DLS before and after DAMGO (0.3 μM, 5 min) and high-frequency stimulation (HFS) coupled with depolarization (4 pulses of 100 Hz, 10 s inter-pulse interval). DAMGO application was incapable of producing mOP-LTD in the DLS of anterior insula MOR knockout mice. However, HFS induced a strong reduction of eEPSCs in the DLS, indicating intact eCB-LTD (baseline vs DAMGO: P = 0.262, t 3 = 1.3.78; baseline vs HFS: P = 0.0082, t 3 = 6.259; DAMGO vs HFS: P = 0.0467, t 3 = 3.273; n = 4 from 3 mice). Data analyzed with Student’s paired t tests. Data represent mean ± SEM

    Article Snippet: Reagents The MOR agonist DAMGO (H-2535, Bachem), MOR antagonist CTAP (H-3698, Bachem), delta opioid receptor agonist [D-Pen2 ,D-Pen5 ]-enkephalin (DPDPE; H-2905m, Bachem), α7 nicotinic acetylcholine receptor antagonist methyllycaconitine citrate (MLA; 1029, Tocris), AMPA antagonist NBQX (0373, Tocris), tetrodotoxin citrate (ARCD-0640, ARC Inc.), EtOH (E7148, Sigma-Aldrich), and GABAA receptor antagonist picrotoxin (P1675, Sigma-Aldrich) were used.

    Techniques: Slice Preparation, Mouse Assay, Plasmid Preparation, Injection, Infection, Expressing, Knock-Out

    mOP-LTD occurs at anterior insular cortex inputs to DLS and is ethanol sensitive. a Schematic figure of the injection paradigm enabling optogenetic recording from C57BL/6J DLS MSNs. An AAV vector coding for ChR2 (AAV.hSyn.ChR2) was injected 14 days prior to recordings. Coronal brain slices showing the infection of anterior insular cortex sending projections to the DLS and nucleus accumbens. Bar scales: +2.4, 200 μm; +1.7, 1000 μm; +1.2, 1000 μm; +0.1, 1000 μm. b Representative light-evoked synaptic traces from the DLS before and after DAMGO (0.3 μM, 5 min) and blocked with MOR antagonist CTAP (1 μM). c , d DAMGO application induced mOP-LTD at anterior insular terminals in the DLS and this MOR-mediated LTD was blocked by the application of CTAP ( P = 0.027, t 13 = 2.49, Control: n = 9 from 3 mice; CTAP: n = 6 from 2 mice). e Representative oEPSC traces from the DLS before and after DAMGO (0.3 μM, 5 min) application in saline (blue traces) and EtOH (red traces)-injected C57BL/6J mice. f , g EtOH exposure produced a disruption of mOP-LTD from anterior insular inputs induced by DAMGO (0.3 μM, 5 min) in the DLS ( P = 0.0046, t 9 = 3.75; Saline: n = 6 from 2 mice; EtOH: n = 5 from 3 mice). Unpaired Student’s t test. * P

    Journal: Nature Communications

    Article Title: Alcohol exposure disrupts mu opioid receptor-mediated long-term depression at insular cortex inputs to dorsolateral striatum

    doi: 10.1038/s41467-018-03683-1

    Figure Lengend Snippet: mOP-LTD occurs at anterior insular cortex inputs to DLS and is ethanol sensitive. a Schematic figure of the injection paradigm enabling optogenetic recording from C57BL/6J DLS MSNs. An AAV vector coding for ChR2 (AAV.hSyn.ChR2) was injected 14 days prior to recordings. Coronal brain slices showing the infection of anterior insular cortex sending projections to the DLS and nucleus accumbens. Bar scales: +2.4, 200 μm; +1.7, 1000 μm; +1.2, 1000 μm; +0.1, 1000 μm. b Representative light-evoked synaptic traces from the DLS before and after DAMGO (0.3 μM, 5 min) and blocked with MOR antagonist CTAP (1 μM). c , d DAMGO application induced mOP-LTD at anterior insular terminals in the DLS and this MOR-mediated LTD was blocked by the application of CTAP ( P = 0.027, t 13 = 2.49, Control: n = 9 from 3 mice; CTAP: n = 6 from 2 mice). e Representative oEPSC traces from the DLS before and after DAMGO (0.3 μM, 5 min) application in saline (blue traces) and EtOH (red traces)-injected C57BL/6J mice. f , g EtOH exposure produced a disruption of mOP-LTD from anterior insular inputs induced by DAMGO (0.3 μM, 5 min) in the DLS ( P = 0.0046, t 9 = 3.75; Saline: n = 6 from 2 mice; EtOH: n = 5 from 3 mice). Unpaired Student’s t test. * P

    Article Snippet: Reagents The MOR agonist DAMGO (H-2535, Bachem), MOR antagonist CTAP (H-3698, Bachem), delta opioid receptor agonist [D-Pen2 ,D-Pen5 ]-enkephalin (DPDPE; H-2905m, Bachem), α7 nicotinic acetylcholine receptor antagonist methyllycaconitine citrate (MLA; 1029, Tocris), AMPA antagonist NBQX (0373, Tocris), tetrodotoxin citrate (ARCD-0640, ARC Inc.), EtOH (E7148, Sigma-Aldrich), and GABAA receptor antagonist picrotoxin (P1675, Sigma-Aldrich) were used.

    Techniques: Injection, Plasmid Preparation, Infection, Mouse Assay, Produced

    MOR activation produces LTD of excitatory transmission in the dorsal striatum. a Schematic figure of coronal brain slice showing the recording of EPSCs evoked by focal electric stimulation in the dorsolateral striatum (DLS) of C57BL/6J mice. b Representative electrically evoked synaptic traces at baseline and after DAMGO (0.3 μM, 5 min) application. c DAMGO induced mOP-LTD of eEPSC amplitude in DLS MSNs of C57BL/6J mice ( n = 7 slices from 4 mice). d The presence of mOP-LTD is not related to alterations in series resistance. e Schematic figure of coronal brain slice showing the recording of eEPSCs by focal electric stimulation in the dorsomedial striatum (DMS). f Representative electrically evoked synaptic traces before and after DAMGO (0.3 μM, 5 min) application. g The activation of MOR by DAMGO induced LTD of eEPSC amplitude in DMS MSNs of C57BL/6J ( n = 6 from 2 mice). h The series resistance was stable during DMS recordings. Data represent mean ± SEM

    Journal: Nature Communications

    Article Title: Alcohol exposure disrupts mu opioid receptor-mediated long-term depression at insular cortex inputs to dorsolateral striatum

    doi: 10.1038/s41467-018-03683-1

    Figure Lengend Snippet: MOR activation produces LTD of excitatory transmission in the dorsal striatum. a Schematic figure of coronal brain slice showing the recording of EPSCs evoked by focal electric stimulation in the dorsolateral striatum (DLS) of C57BL/6J mice. b Representative electrically evoked synaptic traces at baseline and after DAMGO (0.3 μM, 5 min) application. c DAMGO induced mOP-LTD of eEPSC amplitude in DLS MSNs of C57BL/6J mice ( n = 7 slices from 4 mice). d The presence of mOP-LTD is not related to alterations in series resistance. e Schematic figure of coronal brain slice showing the recording of eEPSCs by focal electric stimulation in the dorsomedial striatum (DMS). f Representative electrically evoked synaptic traces before and after DAMGO (0.3 μM, 5 min) application. g The activation of MOR by DAMGO induced LTD of eEPSC amplitude in DMS MSNs of C57BL/6J ( n = 6 from 2 mice). h The series resistance was stable during DMS recordings. Data represent mean ± SEM

    Article Snippet: Reagents The MOR agonist DAMGO (H-2535, Bachem), MOR antagonist CTAP (H-3698, Bachem), delta opioid receptor agonist [D-Pen2 ,D-Pen5 ]-enkephalin (DPDPE; H-2905m, Bachem), α7 nicotinic acetylcholine receptor antagonist methyllycaconitine citrate (MLA; 1029, Tocris), AMPA antagonist NBQX (0373, Tocris), tetrodotoxin citrate (ARCD-0640, ARC Inc.), EtOH (E7148, Sigma-Aldrich), and GABAA receptor antagonist picrotoxin (P1675, Sigma-Aldrich) were used.

    Techniques: Activation Assay, Transmission Assay, Slice Preparation, Mouse Assay

    Modeling mu opioid receptor modulation in EMLO-derived neuronal cultures. a , TUJ1/OPRM1 IF in day 22 H3.3.1 EMLO. High magnification images provided (bottom-left) with multi-dimensional view of gut tube (bottom-right). b , Top: OPRM1 expression in apical aspect of neural rosettes and basal neurons. Bottom: TFAP2α expression at the basal aspect of GABAergic rosettes. c , Fluo-4 AM in dissociated EMLO cultures. High magnification image with example soma ROI (right). d , 2D adherent spinal sensory neurons (top, TUJ1/BRN3A) and spinal motor neurons (bottom, TUJ1/Nkx-6.1) used as controls for opioid-responsive firing. e , Examples of calcium transients quantified in dissociated EMLO neuronal soma using Fluo-4 AM. Shown are no calcium transients (none), one transient (single), or multiple transients (multiple) within a 1.5 min acquisition window. f , Histogram of percent of neurons with multiple calcium transients. EMLO dissociated cultures were compared to spinal sensory neurons (positive control) and spinal motor neurons (negative control). Baseline firing in BrainPhys was compared to addition of 1 μM DAMGO, followed by 10 μM Naloxone in the same cultures. n = number of neurons quantified. Individual scale bars provided. Data reported as (mean ±s.e.m.).

    Journal: bioRxiv

    Article Title: Integrating central and peripheral neurons in elongating multi-lineage-organized gastruloids

    doi: 10.1101/2020.12.29.424774

    Figure Lengend Snippet: Modeling mu opioid receptor modulation in EMLO-derived neuronal cultures. a , TUJ1/OPRM1 IF in day 22 H3.3.1 EMLO. High magnification images provided (bottom-left) with multi-dimensional view of gut tube (bottom-right). b , Top: OPRM1 expression in apical aspect of neural rosettes and basal neurons. Bottom: TFAP2α expression at the basal aspect of GABAergic rosettes. c , Fluo-4 AM in dissociated EMLO cultures. High magnification image with example soma ROI (right). d , 2D adherent spinal sensory neurons (top, TUJ1/BRN3A) and spinal motor neurons (bottom, TUJ1/Nkx-6.1) used as controls for opioid-responsive firing. e , Examples of calcium transients quantified in dissociated EMLO neuronal soma using Fluo-4 AM. Shown are no calcium transients (none), one transient (single), or multiple transients (multiple) within a 1.5 min acquisition window. f , Histogram of percent of neurons with multiple calcium transients. EMLO dissociated cultures were compared to spinal sensory neurons (positive control) and spinal motor neurons (negative control). Baseline firing in BrainPhys was compared to addition of 1 μM DAMGO, followed by 10 μM Naloxone in the same cultures. n = number of neurons quantified. Individual scale bars provided. Data reported as (mean ±s.e.m.).

    Article Snippet: After imaging baseline activity in BrainPhys, 1 μM DAMGO (MOR agonist, 10 mM stock in water; Abcam) was added directly to chamber wells and imaged again.

    Techniques: Derivative Assay, Expressing, Positive Control, Negative Control

    Endothelin effects on channel mutants A , diagrams depict channel mutants: Kir3.4 (S143T) parent, N-terminal truncation, and chimeras. We produced the Kir3.4(S143T) using a cDNA template for cRNA coding a Kir3.4(S143T) having a truncated (1–57) N terminus. We used Kir3 chimeras: Kir3.4(S143T)-(1–338)/Kir3.1-(333–501) and Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). B , oocytes were injected with 1 ng of MOR and 1 ng of HETAR, and either 1 ng of Kir3.4(S143T), 1 ng of Kir3.4(S143T)-(Δ1–57), 1 ng of Kir3.4(S143T)-(1–338)/Kir3.1-(333–501), or 1 ng of Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). The percent inhibition of the second mu opioid response after Et-1 pretreatment is shown. The bar graph summarizes the effects of Et-1 on the DAMGO activation of MOR compared with untreated controls from the same batch. Data are means ± S.E. from four to seven oocytes and two to three independent experiments.

    Journal: The Journal of biological chemistry

    Article Title: Eicosanoids Inhibit the G-protein-gated Inwardly Rectifying Potassium Channel (Kir3) at the Na+/PIP2 Gating Site *

    doi: 10.1074/jbc.M010097200

    Figure Lengend Snippet: Endothelin effects on channel mutants A , diagrams depict channel mutants: Kir3.4 (S143T) parent, N-terminal truncation, and chimeras. We produced the Kir3.4(S143T) using a cDNA template for cRNA coding a Kir3.4(S143T) having a truncated (1–57) N terminus. We used Kir3 chimeras: Kir3.4(S143T)-(1–338)/Kir3.1-(333–501) and Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). B , oocytes were injected with 1 ng of MOR and 1 ng of HETAR, and either 1 ng of Kir3.4(S143T), 1 ng of Kir3.4(S143T)-(Δ1–57), 1 ng of Kir3.4(S143T)-(1–338)/Kir3.1-(333–501), or 1 ng of Kir3.4(S143T)-(1–249)/Kir3.1-(244–501). The percent inhibition of the second mu opioid response after Et-1 pretreatment is shown. The bar graph summarizes the effects of Et-1 on the DAMGO activation of MOR compared with untreated controls from the same batch. Data are means ± S.E. from four to seven oocytes and two to three independent experiments.

    Article Snippet: Endothelin-1 and DAMGO were obtained from Phoenix Pharmaceuticals, Belmont, CA and were stored at −20 °C until use.

    Techniques: Produced, Injection, Inhibition, Activation Assay

    Unilateral dialysis during the day of 100μM DAMGO (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.

    Journal: Respiratory physiology & neurobiology

    Article Title: Effects on breathing of agonists to μ-opioid or GABAA receptors dialyzed into the Ventral Respiratory Column of awake and sleeping goats

    doi: 10.1016/j.resp.2017.01.007

    Figure Lengend Snippet: Unilateral dialysis during the day of 100μM DAMGO (n=9, filled circles) did not significantly ( P ≥0.758) alter ventilation (V̇ I , panel A), breathing frequency (f, panel B) or tidal volume (V T , panel C) compared to dialysis of mCSF alone (n=7, open circles). Data are means ± SE. The x Axis is time from start of 180 minutes of dialysis. As indicated by the black line, 100μM DAMGO was dialyzed between 60 and 120 minutes. The values shown during and after DAMGO dialyses are the percent of the last 15 minutes prior to DAMGO dialyses. F and P values are the interaction term obtained from two-way repeated measures ANOVA using time and dose as factors. Note the trend of a transient reduction in V̇ I and f over the last 30 minutes of DAMGO dialysis.

    Article Snippet: During studies, the perfusate was either mock cerebral spinal fluid (mCSF: 124mM NaCl, 2.0mM KCL, 2.0mM MgCl2 , 1.3mM K2 PO4 , 2.0mM CaCl2 , 11mM glucose, 26mM NaHCO3 − and pH 7.32 in sterile distilled H2O) alone or with the μ-opioid agonist DAMGO (10, 50 or 100μM, Sigma-Aldrich: E7384) or the GABAA agonist muscimol (0.5, 1.0, or 10.0mM, Abcam: ab120094).

    Techniques:

    Visual inspection of ventilatory tracings indicates variability of breathing increased and inspiratory time decreased during and after bilateral dialysis of 100μM DAMGO. The four tracings were from a single goat for a portion of the last 15 minutes of the predialysis control period (panel A) and the last 15 minutes of each of three hours of mCSF dialysis (panels B-D) with DAMGO increased during the second of the three hours (Panel C).

    Journal: Respiratory physiology & neurobiology

    Article Title: Effects on breathing of agonists to μ-opioid or GABAA receptors dialyzed into the Ventral Respiratory Column of awake and sleeping goats

    doi: 10.1016/j.resp.2017.01.007

    Figure Lengend Snippet: Visual inspection of ventilatory tracings indicates variability of breathing increased and inspiratory time decreased during and after bilateral dialysis of 100μM DAMGO. The four tracings were from a single goat for a portion of the last 15 minutes of the predialysis control period (panel A) and the last 15 minutes of each of three hours of mCSF dialysis (panels B-D) with DAMGO increased during the second of the three hours (Panel C).

    Article Snippet: During studies, the perfusate was either mock cerebral spinal fluid (mCSF: 124mM NaCl, 2.0mM KCL, 2.0mM MgCl2 , 1.3mM K2 PO4 , 2.0mM CaCl2 , 11mM glucose, 26mM NaHCO3 − and pH 7.32 in sterile distilled H2O) alone or with the μ-opioid agonist DAMGO (10, 50 or 100μM, Sigma-Aldrich: E7384) or the GABAA agonist muscimol (0.5, 1.0, or 10.0mM, Abcam: ab120094).

    Techniques:

    Membrane potential regulates μ receptor‐induced K ir 3.X currents in HEK293T cells. (a) Representative recording (out of n = 6) of inward K + currents in HEK293T cells expressing wild‐type μ receptors (MOP‐wt) and K ir 3.X channels is shown. K ir 3.X currents were evoked by 4.5 nM morphine (Mor) and 30 nM DAMGO and measured at −90 and −20 mV (voltage protocol is depicted at the bottom; note that depolarization to −20 mV shifts both basal and active currents due to the current–voltage relationship [see Figure S1 ] of the channel). Levels that were used for calculation of maximum responses are shown as light grey line (−90 mV) or dark grey line (−20 mV), and amplitude height is shown by boxes (morphine response: filled box; maximum DAMGO response: empty box). (b) K ir 3.X current responses evoked by non‐saturating morphine concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 6, for further explanation of evaluation, see Section 2 ). (c) Representative recording (out of n = 7) of inward K + currents. K ir 3.X currents were evoked by 3 nM morphine and 30 nM DAMGO and measured and evaluated as explained in (a) (non‐saturating DAMGO response: filled box; saturating response: empty box). (d) K ir 3.X current responses evoked by non‐saturating DAMGO concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 7, for further explanation of evaluation, see Section 2 ). Responses at −90 and −20 mV were compared in the same recording. * P

    Journal: British Journal of Pharmacology

    Article Title: Voltage modulates the effect of μ‐receptor activation in a ligand‐dependent manner. Voltage modulates the effect of μ‐receptor activation in a ligand‐dependent manner

    doi: 10.1111/bph.15070

    Figure Lengend Snippet: Membrane potential regulates μ receptor‐induced K ir 3.X currents in HEK293T cells. (a) Representative recording (out of n = 6) of inward K + currents in HEK293T cells expressing wild‐type μ receptors (MOP‐wt) and K ir 3.X channels is shown. K ir 3.X currents were evoked by 4.5 nM morphine (Mor) and 30 nM DAMGO and measured at −90 and −20 mV (voltage protocol is depicted at the bottom; note that depolarization to −20 mV shifts both basal and active currents due to the current–voltage relationship [see Figure S1 ] of the channel). Levels that were used for calculation of maximum responses are shown as light grey line (−90 mV) or dark grey line (−20 mV), and amplitude height is shown by boxes (morphine response: filled box; maximum DAMGO response: empty box). (b) K ir 3.X current responses evoked by non‐saturating morphine concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 6, for further explanation of evaluation, see Section 2 ). (c) Representative recording (out of n = 7) of inward K + currents. K ir 3.X currents were evoked by 3 nM morphine and 30 nM DAMGO and measured and evaluated as explained in (a) (non‐saturating DAMGO response: filled box; saturating response: empty box). (d) K ir 3.X current responses evoked by non‐saturating DAMGO concentrations were normalized to the maximum response (evoked by a saturating DAMGO concentration) at respective membrane potentials ( n = 7, for further explanation of evaluation, see Section 2 ). Responses at −90 and −20 mV were compared in the same recording. * P

    Article Snippet: 2.12 Materials For HEK293T cell experiments, morphine hydrochloride was purchased from Merck, DAMGO acetate salt, [Met5 ]enkephalin acetate salt and fentanyl citrate were purchased from Sigma Aldrich.

    Techniques: Expressing, Concentration Assay

    The observed voltage sensitivity occurs also in physiological K + concentrations . (a) Representative recording ( n = 7) of outward K + currents measured in HEK293T cells expressing wild‐type μ receptors (MOP‐wt) and K ir 3.4 channels. K ir 3.X currents were evoked by 22.5 nM morphine (Mor; non‐saturating, also see Section 2 ) and 30 nM DAMGO (saturating) and measured at −50 and 0 mV. Levels that were used for calculation of maximum responses are depicted as light grey line (−50 mV) or dark grey line (0 mV), and amplitude height is shown by boxes (morphine response: filled box; saturating DAMGO response: empty box). Voltage protocol is depicted at the bottom; note that depolarization steps shift both basal and active currents due to the current–voltage relationship of the channel (see Figure S2 ). (b) K ir 3.X current responses evoked by non‐saturating morphine concentrations were normalized to the maximum DAMGO response at respective membrane potentials ( n = 7, for further explanation of evaluation, see Section 2 ). Responses at −50 and 0 mV were compared in the same recording. * P

    Journal: British Journal of Pharmacology

    Article Title: Voltage modulates the effect of μ‐receptor activation in a ligand‐dependent manner. Voltage modulates the effect of μ‐receptor activation in a ligand‐dependent manner

    doi: 10.1111/bph.15070

    Figure Lengend Snippet: The observed voltage sensitivity occurs also in physiological K + concentrations . (a) Representative recording ( n = 7) of outward K + currents measured in HEK293T cells expressing wild‐type μ receptors (MOP‐wt) and K ir 3.4 channels. K ir 3.X currents were evoked by 22.5 nM morphine (Mor; non‐saturating, also see Section 2 ) and 30 nM DAMGO (saturating) and measured at −50 and 0 mV. Levels that were used for calculation of maximum responses are depicted as light grey line (−50 mV) or dark grey line (0 mV), and amplitude height is shown by boxes (morphine response: filled box; saturating DAMGO response: empty box). Voltage protocol is depicted at the bottom; note that depolarization steps shift both basal and active currents due to the current–voltage relationship of the channel (see Figure S2 ). (b) K ir 3.X current responses evoked by non‐saturating morphine concentrations were normalized to the maximum DAMGO response at respective membrane potentials ( n = 7, for further explanation of evaluation, see Section 2 ). Responses at −50 and 0 mV were compared in the same recording. * P

    Article Snippet: 2.12 Materials For HEK293T cell experiments, morphine hydrochloride was purchased from Merck, DAMGO acetate salt, [Met5 ]enkephalin acetate salt and fentanyl citrate were purchased from Sigma Aldrich.

    Techniques: Expressing

    DAMGO-induced activation of [ 35 S]- GTPγS binding in P450-deficient and control mouse brains. A) Membranes prepared from control (WT) and Null whole brains were incubated with [ 35 S]-GTPγS and the specified concentrations of DAMGO (abscissa, log M), then filtered as described. Specifically bound [ 35 S]- GTPγS values (ordinate, % of basal binding, mean ± S.E.M.) are shown for 3 male subjects from each genotype. Basal binding (in the absence of DAMGO) was 204.4 ± 34.4 and 180.8 ± 4.6 fmol/mg protein (mean ± S.E.M.) for WT and Null , respectively, not significantly different from each other. B) [ 35 S]-GTPγS binding values are shown (as in A) for membranes incubated with DAMGO (10 µM) for seven specified CNS regions from five male subjects of each genotype. Basal binding values (mean ± S.E.M.) ranged from 87.9 ± 10.3 and 64.5 ± 9.9 (WT, Null , respectively for spinal cord) to 215.9 ± 16.0 and 228.0 ± 60.0 (WT, Null , respectively for neocortex). ANOVA of basal binding values found significant (P

    Journal: Brain research

    Article Title: Neuronal Cytochrome P450 Activity and Opioid Analgesia: Relevant Sites and Mechanisms

    doi: 10.1016/j.brainres.2015.04.045

    Figure Lengend Snippet: DAMGO-induced activation of [ 35 S]- GTPγS binding in P450-deficient and control mouse brains. A) Membranes prepared from control (WT) and Null whole brains were incubated with [ 35 S]-GTPγS and the specified concentrations of DAMGO (abscissa, log M), then filtered as described. Specifically bound [ 35 S]- GTPγS values (ordinate, % of basal binding, mean ± S.E.M.) are shown for 3 male subjects from each genotype. Basal binding (in the absence of DAMGO) was 204.4 ± 34.4 and 180.8 ± 4.6 fmol/mg protein (mean ± S.E.M.) for WT and Null , respectively, not significantly different from each other. B) [ 35 S]-GTPγS binding values are shown (as in A) for membranes incubated with DAMGO (10 µM) for seven specified CNS regions from five male subjects of each genotype. Basal binding values (mean ± S.E.M.) ranged from 87.9 ± 10.3 and 64.5 ± 9.9 (WT, Null , respectively for spinal cord) to 215.9 ± 16.0 and 228.0 ± 60.0 (WT, Null , respectively for neocortex). ANOVA of basal binding values found significant (P

    Article Snippet: Tris, HCl, MgCl2 , EGTA, NaCl, guanosine-5’-diphosphate sodium salt, BSA, adenosine deaminase, guanosine 5′-O-(3-thiotriphosphate) tetralithium salt (GTPγS) and DAMGO acetate were purchased from Sigma Aldrich (St. Louis, MO).

    Techniques: Activation Assay, Binding Assay, Incubation