Bicuculline antagonizes 5-HT(3A) and alpha2 glycine receptors expressed in Xenopus oocytes.
Bicuculline antagonizes 5-HT(3A) and alpha2 glycine receptors expressed in Xenopus oocytes.
复制标题
Bicuculline 拮抗非洲爪蟾卵母细胞中表达的 5-HT(3A) 和 α2 甘氨酸受体。
DOI：
10.1016/s0014-2999(00)00083-2
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发表时间：
2000
影响因子：
5
通讯作者：
Machu,TK
中科院分区：
文献类型：
--
作者：
Sun,H;Machu,TK
The present study examined the effects of bicuculline on the mouse 5-hydroxytryptamine3Areceptor (5-HT3Areceptor and the human α2 subunit of the glycine receptor. Bicuculline antagonized both the 5-HT3Areceptor (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-HT3Aand α2 glycine receptors, respectively, as bicuculline concentrations were increased. A competitive nature of antagonism by bicuculline at the 5-HT3Areceptor was also suggested by displacement of the competitive antagonist, [3H]GR65630 in SF21 insect cells expressing the 5-HT3Areceptor (Ki=19.01±0.71 μ M). Our data and that of others reveal that bicuculline, a purported selective antagonist of the GABAAreceptor, antagonizes at least one receptor subclass in every member of the superfamily of ligand-gated ion channels.
