human β3 receptor Search Results


gaba receptor subunit constructs human β3 dna in pgemhe  (Lundbeck)
90
Lundbeck gaba receptor subunit constructs human β3 dna in pgemhe
2′MeO6MF is a positive modulator of <t>α1-containing</t> GABAA receptors expressed in Xenopus oocytes. (A) Representative current trace showing the potentiation of <t>GABA</t> (EC10: 10 µM) by various concentrations of 2′MeO6MF (1, 10, 30, 100 and 300 µM) at human recombinant α1β2γ2L GABAA receptors. Horizontal bars show the duration of drug application. In the absence of GABA, 2′MeO6MF (300 µM) produced ≍2% of the current produced by the maximum GABA concentration. Note the rebound current following removal of 2′MeO6MF (indicated by the arrows) (B) 2′MeO6MF potentiates the response to GABA (EC10) at recombinant α1β2, α1β1γ2, α1β2γ2L and α1β3γ2L receptors expressed in oocytes. Control GABA concentration at each receptor subtype was 10 µM. Data are mean ± SEM (n = 3–6 oocytes). (C) Representative current trace from an oocyte showing potentiation of GABA (10 µM) by 2′MeO6MF (100 µM) at recombinant α1β2γ2L GABAA receptors. As shown, the enhancement of GABA (10 µM) by 2′MeO6MF (100 µM) was not inhibited by flumazenil (1 and 10 µM) whereas potentiation of GABA (10 µM) by diazepam (1 µM) was inhibited by flumazenil (1 and 10 µM). Horizontal bars show the duration of drug application.
Gaba Receptor Subunit Constructs Human β3 Dna In Pgemhe, supplied by Lundbeck, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/gaba receptor subunit constructs human β3 dna in pgemhe/product/Lundbeck
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gaba receptor subunit constructs human β3 dna in pgemhe - by Bioz Stars, 2026-03
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plasmids encoding wild-type human kir1.1, kir3.2, kir4.1, kir4.2, kir5.1, gabaa receptors (α1, α5, β3, γ2)  (Beijing Genomics Institute Shenzhen)
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Beijing Genomics Institute Shenzhen plasmids encoding wild-type human kir1.1, kir3.2, kir4.1, kir4.2, kir5.1, gabaa receptors (α1, α5, β3, γ2)
2′MeO6MF is a positive modulator of <t>α1-containing</t> GABAA receptors expressed in Xenopus oocytes. (A) Representative current trace showing the potentiation of <t>GABA</t> (EC10: 10 µM) by various concentrations of 2′MeO6MF (1, 10, 30, 100 and 300 µM) at human recombinant α1β2γ2L GABAA receptors. Horizontal bars show the duration of drug application. In the absence of GABA, 2′MeO6MF (300 µM) produced ≍2% of the current produced by the maximum GABA concentration. Note the rebound current following removal of 2′MeO6MF (indicated by the arrows) (B) 2′MeO6MF potentiates the response to GABA (EC10) at recombinant α1β2, α1β1γ2, α1β2γ2L and α1β3γ2L receptors expressed in oocytes. Control GABA concentration at each receptor subtype was 10 µM. Data are mean ± SEM (n = 3–6 oocytes). (C) Representative current trace from an oocyte showing potentiation of GABA (10 µM) by 2′MeO6MF (100 µM) at recombinant α1β2γ2L GABAA receptors. As shown, the enhancement of GABA (10 µM) by 2′MeO6MF (100 µM) was not inhibited by flumazenil (1 and 10 µM) whereas potentiation of GABA (10 µM) by diazepam (1 µM) was inhibited by flumazenil (1 and 10 µM). Horizontal bars show the duration of drug application.
Plasmids Encoding Wild Type Human Kir1.1, Kir3.2, Kir4.1, Kir4.2, Kir5.1, Gabaa Receptors (α1, α5, β3, γ2), supplied by Beijing Genomics Institute Shenzhen, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/plasmids encoding wild-type human kir1.1, kir3.2, kir4.1, kir4.2, kir5.1, gabaa receptors (α1, α5, β3, γ2)/product/Beijing Genomics Institute Shenzhen
Average 90 stars, based on 1 article reviews
plasmids encoding wild-type human kir1.1, kir3.2, kir4.1, kir4.2, kir5.1, gabaa receptors (α1, α5, β3, γ2) - by Bioz Stars, 2026-03
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2′MeO6MF is a positive modulator of α1-containing GABAA receptors expressed in Xenopus oocytes. (A) Representative current trace showing the potentiation of GABA (EC10: 10 µM) by various concentrations of 2′MeO6MF (1, 10, 30, 100 and 300 µM) at human recombinant α1β2γ2L GABAA receptors. Horizontal bars show the duration of drug application. In the absence of GABA, 2′MeO6MF (300 µM) produced ≍2% of the current produced by the maximum GABA concentration. Note the rebound current following removal of 2′MeO6MF (indicated by the arrows) (B) 2′MeO6MF potentiates the response to GABA (EC10) at recombinant α1β2, α1β1γ2, α1β2γ2L and α1β3γ2L receptors expressed in oocytes. Control GABA concentration at each receptor subtype was 10 µM. Data are mean ± SEM (n = 3–6 oocytes). (C) Representative current trace from an oocyte showing potentiation of GABA (10 µM) by 2′MeO6MF (100 µM) at recombinant α1β2γ2L GABAA receptors. As shown, the enhancement of GABA (10 µM) by 2′MeO6MF (100 µM) was not inhibited by flumazenil (1 and 10 µM) whereas potentiation of GABA (10 µM) by diazepam (1 µM) was inhibited by flumazenil (1 and 10 µM). Horizontal bars show the duration of drug application.

Journal: British Journal of Pharmacology

Article Title: 2?-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA A receptors

doi: 10.1111/j.1476-5381.2011.01604.x

Figure Lengend Snippet: 2′MeO6MF is a positive modulator of α1-containing GABAA receptors expressed in Xenopus oocytes. (A) Representative current trace showing the potentiation of GABA (EC10: 10 µM) by various concentrations of 2′MeO6MF (1, 10, 30, 100 and 300 µM) at human recombinant α1β2γ2L GABAA receptors. Horizontal bars show the duration of drug application. In the absence of GABA, 2′MeO6MF (300 µM) produced ≍2% of the current produced by the maximum GABA concentration. Note the rebound current following removal of 2′MeO6MF (indicated by the arrows) (B) 2′MeO6MF potentiates the response to GABA (EC10) at recombinant α1β2, α1β1γ2, α1β2γ2L and α1β3γ2L receptors expressed in oocytes. Control GABA concentration at each receptor subtype was 10 µM. Data are mean ± SEM (n = 3–6 oocytes). (C) Representative current trace from an oocyte showing potentiation of GABA (10 µM) by 2′MeO6MF (100 µM) at recombinant α1β2γ2L GABAA receptors. As shown, the enhancement of GABA (10 µM) by 2′MeO6MF (100 µM) was not inhibited by flumazenil (1 and 10 µM) whereas potentiation of GABA (10 µM) by diazepam (1 µM) was inhibited by flumazenil (1 and 10 µM). Horizontal bars show the duration of drug application.

Article Snippet: GABA receptor subunit constructs Human α1, α2, β2 and γ2L DNA in pcDM8 were provided by Dr Paul Whiting (Merck, Sharpe and Dohme Research Labs, Harlow, UK), α3 and β3 in pGEMHE, α5 in pcDNA3 and β1 in PCDM8 were a gift from Dr Bjarke Ebert (H. Lundbeck A/S, Valby, Denmark).

Techniques: Recombinant, Produced, Concentration Assay, Control

The effects of 2′MeO6MF at the various recombinant ionotropic GABA receptor subtypes expressed in Xenopus oocytes

Journal: British Journal of Pharmacology

Article Title: 2?-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA A receptors

doi: 10.1111/j.1476-5381.2011.01604.x

Figure Lengend Snippet: The effects of 2′MeO6MF at the various recombinant ionotropic GABA receptor subtypes expressed in Xenopus oocytes

Article Snippet: GABA receptor subunit constructs Human α1, α2, β2 and γ2L DNA in pcDM8 were provided by Dr Paul Whiting (Merck, Sharpe and Dohme Research Labs, Harlow, UK), α3 and β3 in pGEMHE, α5 in pcDNA3 and β1 in PCDM8 were a gift from Dr Bjarke Ebert (H. Lundbeck A/S, Valby, Denmark).

Techniques: Recombinant

2′MeO6MF directly activates human recombinant α2β2/3γ2L and α2β2/3 GABAA receptors expressed in oocytes. (A) Current trace showing the effects of increasing concentrations of 2′MeO6MF on recombinant α2β2γ2L GABAA receptors expressed in Xenopus oocytes against the maximum effect of GABA (3000 µM). Horizontal bars indicate duration of drug application. (B) Representative trace showing the potentiation of GABA (EC10: 5 µM) in the presence of diazepam (1 µM) and this effect was attenuated by flumazenil (10 µM) at α2β2γ2L GABAA receptors. In contrast, the direct activation of 2′MeO6MF (30 µM) on the same receptor was not attenuated by flumazenil (10 µM). (C) Representative trace showing that a 3 min pre-incubation with bicuculline (10 µM) attenuates the response produced by 2′MeO6MF (100 µM) by 56 ± 4% at α2β2γ2L GABAA receptors. Gabazine (10 µM and 100 µM) also attenuated the response produced by 2′MeO6MF on α2β2γ2L GABAA receptors by 45 ± 4% and 100% respectively. (D) Concentration–response curves for 2′MeO6MF alone and 2′MeO6MF in the presence of bicuculline (10 µM) and gabazine (1 µM) at α2β2γ2L GABAA receptors expressed in Xenopus oocytes. Data are mean ± SEM (n = 4–6 oocytes). (E) Concentration–response curves for 2′MeO6MF on α2β3γ2L, α2β2γ2L, α2β3 and α2β2 recombinant GABAA receptors expressed in oocytes. Currents are expressed as a percentage of the peak current elicited by 3 mM GABA. Data are mean ± SEM (n = 4–6 oocytes).

Journal: British Journal of Pharmacology

Article Title: 2?-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA A receptors

doi: 10.1111/j.1476-5381.2011.01604.x

Figure Lengend Snippet: 2′MeO6MF directly activates human recombinant α2β2/3γ2L and α2β2/3 GABAA receptors expressed in oocytes. (A) Current trace showing the effects of increasing concentrations of 2′MeO6MF on recombinant α2β2γ2L GABAA receptors expressed in Xenopus oocytes against the maximum effect of GABA (3000 µM). Horizontal bars indicate duration of drug application. (B) Representative trace showing the potentiation of GABA (EC10: 5 µM) in the presence of diazepam (1 µM) and this effect was attenuated by flumazenil (10 µM) at α2β2γ2L GABAA receptors. In contrast, the direct activation of 2′MeO6MF (30 µM) on the same receptor was not attenuated by flumazenil (10 µM). (C) Representative trace showing that a 3 min pre-incubation with bicuculline (10 µM) attenuates the response produced by 2′MeO6MF (100 µM) by 56 ± 4% at α2β2γ2L GABAA receptors. Gabazine (10 µM and 100 µM) also attenuated the response produced by 2′MeO6MF on α2β2γ2L GABAA receptors by 45 ± 4% and 100% respectively. (D) Concentration–response curves for 2′MeO6MF alone and 2′MeO6MF in the presence of bicuculline (10 µM) and gabazine (1 µM) at α2β2γ2L GABAA receptors expressed in Xenopus oocytes. Data are mean ± SEM (n = 4–6 oocytes). (E) Concentration–response curves for 2′MeO6MF on α2β3γ2L, α2β2γ2L, α2β3 and α2β2 recombinant GABAA receptors expressed in oocytes. Currents are expressed as a percentage of the peak current elicited by 3 mM GABA. Data are mean ± SEM (n = 4–6 oocytes).

Article Snippet: GABA receptor subunit constructs Human α1, α2, β2 and γ2L DNA in pcDM8 were provided by Dr Paul Whiting (Merck, Sharpe and Dohme Research Labs, Harlow, UK), α3 and β3 in pGEMHE, α5 in pcDNA3 and β1 in PCDM8 were a gift from Dr Bjarke Ebert (H. Lundbeck A/S, Valby, Denmark).

Techniques: Recombinant, Activation Assay, Incubation, Produced, Concentration Assay

(A) Representative trace showing the activation of 2′MeO6MF (300 µM) is significantly reduced at the mutant α2β2N265Sγ2L GABAA receptor. In contrast, 2′MeO6MF (300 µM) was able to positively modulate GABA (10 µM) by 454 ± 16%. Horizontal bars show duration of drug application. (B) Concentration–response curves for 2′MeO6MF in the presence of GABA (EC10) at α2β1, α2β1γ2L and α2β2N265Sγ2L. Control GABA dose was 10 µM. Data are mean ± SEM (n = 4 oocytes). (C) Representative trace showing 2′MeO6MF (100 µM) directly activating recombinant α2β1S265Nγ2L mutant GABAA receptors. The current generated by 2′MeO6MF (100 µM) in the presence of GABA (10 µM) is the sum of the individual currents produced by GABA (10 µM) and 2′MeO6MF (100 µM) alone. Horizontal bars show duration of drug application. (D) Concentration–response curve for 2′MeO6MF expressed relative the maximal GABA concentration (3 mM) at α2β1S265Nγ2L GABAA receptors showing that the converse mutation converted 2′MeO6MF from a potentiator to a direct activator. Data are mean ± SEM for three to four oocytes.

Journal: British Journal of Pharmacology

Article Title: 2?-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA A receptors

doi: 10.1111/j.1476-5381.2011.01604.x

Figure Lengend Snippet: (A) Representative trace showing the activation of 2′MeO6MF (300 µM) is significantly reduced at the mutant α2β2N265Sγ2L GABAA receptor. In contrast, 2′MeO6MF (300 µM) was able to positively modulate GABA (10 µM) by 454 ± 16%. Horizontal bars show duration of drug application. (B) Concentration–response curves for 2′MeO6MF in the presence of GABA (EC10) at α2β1, α2β1γ2L and α2β2N265Sγ2L. Control GABA dose was 10 µM. Data are mean ± SEM (n = 4 oocytes). (C) Representative trace showing 2′MeO6MF (100 µM) directly activating recombinant α2β1S265Nγ2L mutant GABAA receptors. The current generated by 2′MeO6MF (100 µM) in the presence of GABA (10 µM) is the sum of the individual currents produced by GABA (10 µM) and 2′MeO6MF (100 µM) alone. Horizontal bars show duration of drug application. (D) Concentration–response curve for 2′MeO6MF expressed relative the maximal GABA concentration (3 mM) at α2β1S265Nγ2L GABAA receptors showing that the converse mutation converted 2′MeO6MF from a potentiator to a direct activator. Data are mean ± SEM for three to four oocytes.

Article Snippet: GABA receptor subunit constructs Human α1, α2, β2 and γ2L DNA in pcDM8 were provided by Dr Paul Whiting (Merck, Sharpe and Dohme Research Labs, Harlow, UK), α3 and β3 in pGEMHE, α5 in pcDNA3 and β1 in PCDM8 were a gift from Dr Bjarke Ebert (H. Lundbeck A/S, Valby, Denmark).

Techniques: Activation Assay, Mutagenesis, Concentration Assay, Control, Recombinant, Generated, Produced