Bicuculline antagonizes 5-HT(3A) and α2 glycine receptors expressed in Xenopus oocytes

Hongwei Sun; Tina K. Machu

doi:10.1016/S0014-2999(00)00083-2

Bicuculline antagonizes 5-HT(3A) and α2 glycine receptors expressed in Xenopus oocytes

Hongwei Sun, Tina K. Machu

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19 Scopus citations

Abstract

The present study examined the effects of bicuculline on the mouse 5-hydroxytryptamine(3A) receptor (5-HT(3A) receptor and the human α2 subunit of the glycine receptor. Bicuculline antagonized both the 5-HT(3A) receptor (IC₅₀=20.12±0.39 μM) and the α2 glycine receptor (IC₅₀=169.40±1.73 μM). A competitive form of antagonism by bicuculline was suggested by experiments in which the EC₅₀s for 5-HT and glycine were increased in the 5-HT(3A) and α2 glycine receptors, respectively, as bicuculline concentrations were increased. A competitive nature of antagonism by bicuculline at the 5-HT(3A) receptor was also suggested by displacement of the competitive antagonist, [³H]GR65630 in SF21 insect cells expressing the 5-HT(3A) receptor (K(i)=19.01±0.71 μ M). Our data and that of others reveal that bicuculline, a purported selective antagonist of the GABA(A) receptor, antagonizes at least one receptor subclass in every member of the superfamily of ligand-gated ion channels. Copyright (C) 2000 Elsevier Science B.V.

Original language	English
Pages (from-to)	243-249
Number of pages	7
Journal	European Journal of Pharmacology
Volume	391
Issue number	3
DOIs	https://doi.org/10.1016/S0014-2999(00)00083-2
State	Published - 17 Mar 2000

Keywords

5-HT receptor
5-HT(5-hydroxytryptamine, serotonin)
Bicuculline
GABA(A)
Nicotinic acetylcholine receptor
glycine receptor

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10.1016/S0014-2999(00)00083-2

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title = "Bicuculline antagonizes 5-HT(3A) and α2 glycine receptors expressed in Xenopus oocytes",

abstract = "The present study examined the effects of bicuculline on the mouse 5-hydroxytryptamine(3A) receptor (5-HT(3A) receptor and the human α2 subunit of the glycine receptor. Bicuculline antagonized both the 5-HT(3A) receptor (IC50=20.12±0.39 μM) and the α2 glycine receptor (IC50=169.40±1.73 μM). A competitive form of antagonism by bicuculline was suggested by experiments in which the EC50s for 5-HT and glycine were increased in the 5-HT(3A) and α2 glycine receptors, respectively, as bicuculline concentrations were increased. A competitive nature of antagonism by bicuculline at the 5-HT(3A) receptor was also suggested by displacement of the competitive antagonist, [3H]GR65630 in SF21 insect cells expressing the 5-HT(3A) receptor (K(i)=19.01±0.71 μ M). Our data and that of others reveal that bicuculline, a purported selective antagonist of the GABA(A) receptor, antagonizes at least one receptor subclass in every member of the superfamily of ligand-gated ion channels. Copyright (C) 2000 Elsevier Science B.V.",

keywords = "5-HT receptor, 5-HT(5-hydroxytryptamine, serotonin), Bicuculline, GABA(A), Nicotinic acetylcholine receptor, glycine receptor",

author = "Hongwei Sun and Machu, {Tina K.}",

note = "Funding Information: This research was supported in part by National Institutes of Health Grand AA10561 (TKM). The contents of this report are solely the responsibility of the authors and do not necessarily represent the views of the aforementioned awarding agencies.",

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AU - Sun, Hongwei

AU - Machu, Tina K.

N1 - Funding Information: This research was supported in part by National Institutes of Health Grand AA10561 (TKM). The contents of this report are solely the responsibility of the authors and do not necessarily represent the views of the aforementioned awarding agencies.

PY - 2000/3/17

Y1 - 2000/3/17

N2 - The present study examined the effects of bicuculline on the mouse 5-hydroxytryptamine(3A) receptor (5-HT(3A) receptor and the human α2 subunit of the glycine receptor. Bicuculline antagonized both the 5-HT(3A) receptor (IC50=20.12±0.39 μM) and the α2 glycine receptor (IC50=169.40±1.73 μM). A competitive form of antagonism by bicuculline was suggested by experiments in which the EC50s for 5-HT and glycine were increased in the 5-HT(3A) and α2 glycine receptors, respectively, as bicuculline concentrations were increased. A competitive nature of antagonism by bicuculline at the 5-HT(3A) receptor was also suggested by displacement of the competitive antagonist, [3H]GR65630 in SF21 insect cells expressing the 5-HT(3A) receptor (K(i)=19.01±0.71 μ M). Our data and that of others reveal that bicuculline, a purported selective antagonist of the GABA(A) receptor, antagonizes at least one receptor subclass in every member of the superfamily of ligand-gated ion channels. Copyright (C) 2000 Elsevier Science B.V.

AB - The present study examined the effects of bicuculline on the mouse 5-hydroxytryptamine(3A) receptor (5-HT(3A) receptor and the human α2 subunit of the glycine receptor. Bicuculline antagonized both the 5-HT(3A) receptor (IC50=20.12±0.39 μM) and the α2 glycine receptor (IC50=169.40±1.73 μM). A competitive form of antagonism by bicuculline was suggested by experiments in which the EC50s for 5-HT and glycine were increased in the 5-HT(3A) and α2 glycine receptors, respectively, as bicuculline concentrations were increased. A competitive nature of antagonism by bicuculline at the 5-HT(3A) receptor was also suggested by displacement of the competitive antagonist, [3H]GR65630 in SF21 insect cells expressing the 5-HT(3A) receptor (K(i)=19.01±0.71 μ M). Our data and that of others reveal that bicuculline, a purported selective antagonist of the GABA(A) receptor, antagonizes at least one receptor subclass in every member of the superfamily of ligand-gated ion channels. Copyright (C) 2000 Elsevier Science B.V.

KW - 5-HT receptor

KW - 5-HT(5-hydroxytryptamine, serotonin)

KW - Bicuculline

KW - GABA(A)

KW - Nicotinic acetylcholine receptor

KW - glycine receptor

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JF - European Journal of Pharmacology

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ER -

Bicuculline antagonizes 5-HT(3A) and α2 glycine receptors expressed in Xenopus oocytes

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