tertiapinq  (Alomone Labs)


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    Name:
    Tertiapin Q
    Description:
    Tertiapin Q blocks a range of inward rectifier K channels Kir in particular ROMK1 and GIRK but with no effect on Kir2 family members In addition it was shown to inhibit acetylcholine induced K currents in heart Tertiapin Q is a derivative of Tertiapin in which Met is replaced by Gln Tertiapin Q inhibits the above mentioned channels with similar affinities
    Catalog Number:
    STT-170
    Price:
    111.0
    Category:
    Toxin
    Source:
    Synthetic peptide
    Applications:
    0
    Purity:
    >98% (HPLC)
    Size:
    0 1 mg
    Format:
    Lyophilized powder.
    Formula:
    C106H175N35O24S4
    Molecular Weight:
    2452 Da.
    Molecule Name:
    Tertiapin-Q
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    Structured Review

    Alomone Labs tertiapinq
    Tertiapin Q
    Tertiapin Q blocks a range of inward rectifier K channels Kir in particular ROMK1 and GIRK but with no effect on Kir2 family members In addition it was shown to inhibit acetylcholine induced K currents in heart Tertiapin Q is a derivative of Tertiapin in which Met is replaced by Gln Tertiapin Q inhibits the above mentioned channels with similar affinities
    https://www.bioz.com/result/tertiapinq/product/Alomone Labs
    Average 92 stars, based on 1 article reviews
    Price from $9.99 to $1999.99
    tertiapinq - by Bioz Stars, 2021-09
    92/100 stars

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    Related Articles

    Recombinant:

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury
    Article Snippet: .. Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. ..

    other:

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury
    Article Snippet: For tertiapin-Q experiments we applied voltage ramps from a holding potential of -40 mV and measured the induced current at -80 mV, based on previously published protocols ( ; ).

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury
    Article Snippet: DAMGO-induced currents in our experiments were diminished by both a general potassium channel blocker barium, and by tertiapin-Q, currently considered the most selective Kir3 channel blocker ( ; ).

    Article Title: Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists
    Article Snippet: Tertiapin-Q was purchased from Alomone Labs.

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury
    Article Snippet: The ramps were applied every 10 s for 200 s in the absence or presence of DAMGO without or with tertiapin-Q.

    Mouse Assay:

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury
    Article Snippet: .. DiscussionIn this study, we found that the MOR-selective agonist DAMGO induces potassium currents in DRG neurons of both naïve mice and mice with CCI of the sciatic nerve, which were diminished by barium and tertiapin-Q indicating the involvement of Kir3 channels. ..

    Mass Spectrometry:

    Article Title: Selective binding of a toxin and phosphatidylinositides to a mammalian potassium channel
    Article Snippet: .. TertiapinQ (Alomone Labs) was directly solubilized in MS-compatible buffer. ..

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  • 92
    Alomone Labs tertiapin q
    DAMGO (10 μM)-induced potassium currents in mouse DRG neurons obtained in the voltage ramp mode. (A) Number of neurons responding and non-responding to DAMGO from naïve and CCI mice. The proportion of DAMGO-responding to DAMGO-non-responding neurons from naïve vs. CCI mice did not differ significantly ( P = 0.596; Fisher’s exact t -test). The neurons were sampled from cultures obtained from DRG of seven naïve and eight CCI mice. (B) Single neuron currents in DAMGO-responders. The data points represent single neuron values, and the red horizontal lines indicate the means. Numbers in brackets indicate the number of neurons. (C–F) Exemplary currents of DRG neurons non-responding (C) and responding (D) to DAMGO from naïve mice, and DRG neurons non-responding (E) and responding (F) to DAMGO from mice on day 2 following CCI. The DAMGO effects are shown before and during <t>tertiapin-Q</t> (100 nM) application. (G,H) Tertiapin-Q (100 nM)-mediated attenuation of DAMGO-induced currents in individual neurons from naïve mice ( n = 8 neurons; ∗ P = 0.0204, paired t -test) (G) and CCI mice ( n = 9 neurons; ∗∗ P = 0.0073, paired t -test) (H) . Only DAMGO-responding neurons are shown. Data points represent DAMGO-induced currents of the same neuron before and after application of tertiapin-Q. Dotted lines represent zero current. In all experiments, the currents were obtained by voltage ramps from a holding potential of –40 mV and measured at –80 mV in high potassium extracellular buffer (45 mM). Neurons were defined as responding to DAMGO if the resulting current was larger than three times the noise range.
    Tertiapin Q, supplied by Alomone Labs, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/tertiapin q/product/Alomone Labs
    Average 92 stars, based on 1 article reviews
    Price from $9.99 to $1999.99
    tertiapin q - by Bioz Stars, 2021-09
    92/100 stars
      Buy from Supplier

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    DAMGO (10 μM)-induced potassium currents in mouse DRG neurons obtained in the voltage ramp mode. (A) Number of neurons responding and non-responding to DAMGO from naïve and CCI mice. The proportion of DAMGO-responding to DAMGO-non-responding neurons from naïve vs. CCI mice did not differ significantly ( P = 0.596; Fisher’s exact t -test). The neurons were sampled from cultures obtained from DRG of seven naïve and eight CCI mice. (B) Single neuron currents in DAMGO-responders. The data points represent single neuron values, and the red horizontal lines indicate the means. Numbers in brackets indicate the number of neurons. (C–F) Exemplary currents of DRG neurons non-responding (C) and responding (D) to DAMGO from naïve mice, and DRG neurons non-responding (E) and responding (F) to DAMGO from mice on day 2 following CCI. The DAMGO effects are shown before and during tertiapin-Q (100 nM) application. (G,H) Tertiapin-Q (100 nM)-mediated attenuation of DAMGO-induced currents in individual neurons from naïve mice ( n = 8 neurons; ∗ P = 0.0204, paired t -test) (G) and CCI mice ( n = 9 neurons; ∗∗ P = 0.0073, paired t -test) (H) . Only DAMGO-responding neurons are shown. Data points represent DAMGO-induced currents of the same neuron before and after application of tertiapin-Q. Dotted lines represent zero current. In all experiments, the currents were obtained by voltage ramps from a holding potential of –40 mV and measured at –80 mV in high potassium extracellular buffer (45 mM). Neurons were defined as responding to DAMGO if the resulting current was larger than three times the noise range.

    Journal: Frontiers in Pharmacology

    Article Title: Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons – Effects of Nerve Injury

    doi: 10.3389/fphar.2018.01478

    Figure Lengend Snippet: DAMGO (10 μM)-induced potassium currents in mouse DRG neurons obtained in the voltage ramp mode. (A) Number of neurons responding and non-responding to DAMGO from naïve and CCI mice. The proportion of DAMGO-responding to DAMGO-non-responding neurons from naïve vs. CCI mice did not differ significantly ( P = 0.596; Fisher’s exact t -test). The neurons were sampled from cultures obtained from DRG of seven naïve and eight CCI mice. (B) Single neuron currents in DAMGO-responders. The data points represent single neuron values, and the red horizontal lines indicate the means. Numbers in brackets indicate the number of neurons. (C–F) Exemplary currents of DRG neurons non-responding (C) and responding (D) to DAMGO from naïve mice, and DRG neurons non-responding (E) and responding (F) to DAMGO from mice on day 2 following CCI. The DAMGO effects are shown before and during tertiapin-Q (100 nM) application. (G,H) Tertiapin-Q (100 nM)-mediated attenuation of DAMGO-induced currents in individual neurons from naïve mice ( n = 8 neurons; ∗ P = 0.0204, paired t -test) (G) and CCI mice ( n = 9 neurons; ∗∗ P = 0.0073, paired t -test) (H) . Only DAMGO-responding neurons are shown. Data points represent DAMGO-induced currents of the same neuron before and after application of tertiapin-Q. Dotted lines represent zero current. In all experiments, the currents were obtained by voltage ramps from a holding potential of –40 mV and measured at –80 mV in high potassium extracellular buffer (45 mM). Neurons were defined as responding to DAMGO if the resulting current was larger than three times the noise range.

    Article Snippet: Discussion In this study, we found that the MOR-selective agonist DAMGO induces potassium currents in DRG neurons of both naïve mice and mice with CCI of the sciatic nerve, which were diminished by barium and tertiapin-Q indicating the involvement of Kir3 channels.

    Techniques: Mouse Assay

    Effects of tertiapin-Q on oxycodone- and morphine-induced K IR 3.1 channel activation in Xenopus oocytes. The data presented are typical recordings of K + channel current by (A) oxycodone and (B) morphine. Representative current responses to oxycodone (100

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Effects of tertiapin-Q on oxycodone- and morphine-induced K IR 3.1 channel activation in Xenopus oocytes. The data presented are typical recordings of K + channel current by (A) oxycodone and (B) morphine. Representative current responses to oxycodone (100

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Activation Assay

    Effects of tertiapin-Q on the antinociceptive effects of morphine and oxycodone

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Effects of tertiapin-Q on the antinociceptive effects of morphine and oxycodone

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques:

    Effects of tertiapin-Q on oxycodone- and morphine-induced antinociceptive effects in the (A) FBC and (B) neuropathic pain models. Groups of mice were treated with tertiapin-Q (30 pmol per mouse, i.c.v.) 10 min before the opioids, and either oxycodone

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Effects of tertiapin-Q on oxycodone- and morphine-induced antinociceptive effects in the (A) FBC and (B) neuropathic pain models. Groups of mice were treated with tertiapin-Q (30 pmol per mouse, i.c.v.) 10 min before the opioids, and either oxycodone

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Mouse Assay

    Dose-dependent antinociceptive effects induced by i.t. administration of oxycodone and morphine in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before the opioids. The

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Dose-dependent antinociceptive effects induced by i.t. administration of oxycodone and morphine in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before the opioids. The

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Mouse Assay, Tail Flick Test

    Effects of tertiapin-Q on the antinociceptive effects of morphine and oxycodone

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Effects of tertiapin-Q on the antinociceptive effects of morphine and oxycodone

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques:

    Dose-dependent antinociceptive effect induced by i.c.v. administration of fentanyl in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before fentanyl. Fentanyl (0.1–1.7

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Dose-dependent antinociceptive effect induced by i.c.v. administration of fentanyl in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before fentanyl. Fentanyl (0.1–1.7

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Mouse Assay, Tail Flick Test

    Dose-dependent antinociceptive effects induced by i.c.v. administration of oxycodone and morphine in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before the opioids. The

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Dose-dependent antinociceptive effects induced by i.c.v. administration of oxycodone and morphine in the presence of tertiapin-Q in mice tail-flick test. Groups of mice were pretreated with tertiapin-Q (30 pmol per mouse) 10 min before the opioids. The

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Mouse Assay, Tail Flick Test

    Effects of tertiapin-Q on oxycodone- and morphine-induced antinociception after i.c.v. administration in mice tail-flick test. Groups of mice were treated with tertiapin-Q (3–30 mol per mouse, i.c.v.) 10 min before the opioids, either oxycodone

    Journal: British Journal of Pharmacology

    Article Title: G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites

    doi: 10.1111/bph.12441

    Figure Lengend Snippet: Effects of tertiapin-Q on oxycodone- and morphine-induced antinociception after i.c.v. administration in mice tail-flick test. Groups of mice were treated with tertiapin-Q (3–30 mol per mouse, i.c.v.) 10 min before the opioids, either oxycodone

    Article Snippet: Tertiapin-Q was purchased from Alomone Labs Ltd. (Jerusalem, Israel), and pertussis toxin (PTX) was purchased from Sigma-Aldrich (Tokyo, Japan).

    Techniques: Mouse Assay, Tail Flick Test

    Expression of GIRK channels in AtT20 cells . Left panel: Currents were measured before (control) and after the addition of somatostatin (200 nM) during voltage steps applied from the holding potential of −40 to −60, −80, and −100 mV. Addition of tertiapin (500 nM) inhibited the current (bottom records). The solid lines represent zero current. Top right panel: I/V relationship for the somatostatin activated current (Som) displayed inward rectification and a reversal potential of −40 mV. Current values were obtained by subtracting the currents by records obtained in the presence of 1 mM BaCl 2 . Each point represents the mean ± SE current (pA/pF) measured in three to five cells. Bottom right panel: dose versus response curve for tertiapin-Q block of the AtT20 cell GIRK current. Each point represents the mean ± SE inhibition obtained from three to six experiments. The calculated IC 50 value for tertiapin-Q block was 60 nM.

    Journal: Frontiers in Pharmacology

    Article Title: Targeting GIRK Channels for the Development of New Therapeutic Agents

    doi: 10.3389/fphar.2011.00064

    Figure Lengend Snippet: Expression of GIRK channels in AtT20 cells . Left panel: Currents were measured before (control) and after the addition of somatostatin (200 nM) during voltage steps applied from the holding potential of −40 to −60, −80, and −100 mV. Addition of tertiapin (500 nM) inhibited the current (bottom records). The solid lines represent zero current. Top right panel: I/V relationship for the somatostatin activated current (Som) displayed inward rectification and a reversal potential of −40 mV. Current values were obtained by subtracting the currents by records obtained in the presence of 1 mM BaCl 2 . Each point represents the mean ± SE current (pA/pF) measured in three to five cells. Bottom right panel: dose versus response curve for tertiapin-Q block of the AtT20 cell GIRK current. Each point represents the mean ± SE inhibition obtained from three to six experiments. The calculated IC 50 value for tertiapin-Q block was 60 nM.

    Article Snippet: Drugs and chemicals Carbachol, somatostatin, and a Na+ , K+ channel modulator kit (catalog # LO2220), containing 68 compounds, were purchased from Sigma-Aldrich Chemical Corp. Tertiapin-Q (synthetic formulation) was obtained from Alomone Labs.

    Techniques: Expressing, Blocking Assay, Inhibition

    Block of GIRK channels by Ba 2+ and tertiapin-Q . Top panel: somatostatin-sensitive fluorescent signal measured in AtT20 cells pretreated for 5 min with either 2 mM BaCl 2 or 500 nM tertiapin-Q. Each point represents the mean ± SE value obtained in six wells in one plate. Bottom panel: dose versus response curve for tertiapin-Q block of the HL-1 cell (carbachol stimulation) or AtT20 cell (somatostatin stimulation) GIRK fluorescent signal. Each point represents the mean ± SE inhibition obtained from three to five experiments. Calculated IC 50 values for tertiapin-Q block were HL-1 cells = 1.4 nM, AtT20 cells = 102 nM.

    Journal: Frontiers in Pharmacology

    Article Title: Targeting GIRK Channels for the Development of New Therapeutic Agents

    doi: 10.3389/fphar.2011.00064

    Figure Lengend Snippet: Block of GIRK channels by Ba 2+ and tertiapin-Q . Top panel: somatostatin-sensitive fluorescent signal measured in AtT20 cells pretreated for 5 min with either 2 mM BaCl 2 or 500 nM tertiapin-Q. Each point represents the mean ± SE value obtained in six wells in one plate. Bottom panel: dose versus response curve for tertiapin-Q block of the HL-1 cell (carbachol stimulation) or AtT20 cell (somatostatin stimulation) GIRK fluorescent signal. Each point represents the mean ± SE inhibition obtained from three to five experiments. Calculated IC 50 values for tertiapin-Q block were HL-1 cells = 1.4 nM, AtT20 cells = 102 nM.

    Article Snippet: Drugs and chemicals Carbachol, somatostatin, and a Na+ , K+ channel modulator kit (catalog # LO2220), containing 68 compounds, were purchased from Sigma-Aldrich Chemical Corp. Tertiapin-Q (synthetic formulation) was obtained from Alomone Labs.

    Techniques: Blocking Assay, Inhibition

    KO inhibition induced by electrical head skin stimulation (arrows) is mediated by GIRKs. A , A voltage-clamp recording shows the slow outward KO current and its onset (inset, *) after KO stimulation (five pulses at 30 Hz). A voltage ramp rising from −100 to 0 mV is applied at the peak of the current. Membrane potential is held at −60 mV at rest. B , I-V data points averaged from five recordings during the voltage ramp in A for estimating the reversal of the currents and their rectification. C , Effects of microperfusing 50 µM Ba 2+ on KO inhibition in a dIN. D , Summary of blockade of peak conductance rises by 50–100 µM Ba 2+ during KO in two dINs and six non-dINs (paired t tests). E , Microperfusing 3 µM Tertiapin-Q (T-Q) weakened the peak conductance increase during KO in one dIN and five non-dINs (paired t tests). F , One dIN recording with a pipette solution containing 10 µM GRK2i at the beginning (control) and after 28 min of equilibration. G , GRK2i weakened the peak conductance increase during KO inhibition ( n = 8, paired t test). H , Summary of peak membrane conductance increase during KO in control and after BAPTA equilibration ( n = 8, related samples Wilcoxon signed rank test, p = 0.33). *, significance at p

    Journal: eNeuro

    Article Title: Mechanosensory Stimulation Evokes Acute Concussion-Like Behavior by Activating GIRKs Coupled to Muscarinic Receptors in a Simple Vertebrate

    doi: 10.1523/ENEURO.0073-17.2017

    Figure Lengend Snippet: KO inhibition induced by electrical head skin stimulation (arrows) is mediated by GIRKs. A , A voltage-clamp recording shows the slow outward KO current and its onset (inset, *) after KO stimulation (five pulses at 30 Hz). A voltage ramp rising from −100 to 0 mV is applied at the peak of the current. Membrane potential is held at −60 mV at rest. B , I-V data points averaged from five recordings during the voltage ramp in A for estimating the reversal of the currents and their rectification. C , Effects of microperfusing 50 µM Ba 2+ on KO inhibition in a dIN. D , Summary of blockade of peak conductance rises by 50–100 µM Ba 2+ during KO in two dINs and six non-dINs (paired t tests). E , Microperfusing 3 µM Tertiapin-Q (T-Q) weakened the peak conductance increase during KO in one dIN and five non-dINs (paired t tests). F , One dIN recording with a pipette solution containing 10 µM GRK2i at the beginning (control) and after 28 min of equilibration. G , GRK2i weakened the peak conductance increase during KO inhibition ( n = 8, paired t test). H , Summary of peak membrane conductance increase during KO in control and after BAPTA equilibration ( n = 8, related samples Wilcoxon signed rank test, p = 0.33). *, significance at p

    Article Snippet: Tertiapin-Q was obtained from Alomone labs and other chemical agents were either from Sigma or Tocris.

    Techniques: Inhibition, Transferring