5-羟色胺1D受体拮抗剂GR 127,935是克隆的人5-羟色胺1Dα受体位点的激动剂。
The 5-HT1D receptor antagonist GR 127,935 is an agonist at cloned human 5-HT1D alpha receptor sites.
作者信息
Pauwels P J, Colpaert F C
机构信息
Centre de Recherche Pierre Fabre, Laboratory of Cellular and Molecular Neurobiology, Castres, France.
出版信息
Neuropharmacology. 1995 Feb;34(2):235-7. doi: 10.1016/0028-3908(95)00007-s.
The cAMP response of the 5-HT1D receptor antagonist GR 127,935 was compared with 5-CT and ketanserin at cloned human 5-HT1D alpha receptor sites in transfected C6-glial cells. GR 127,935 showed marked agonist activity (EC50-value: 141 nM), its maximal effect being comparable to that of the agonist 5-CT (EC50-value: 0.91 nM), unlike the apparently silent antagonist ketanserin (KB-value: 34 nM).
在转染的C6神经胶质细胞中，将5-HT1D受体拮抗剂GR 127,935与5-CT和酮色林在克隆的人5-HT1Dα受体位点上的环磷酸腺苷（cAMP）反应进行了比较。GR 127,935表现出显著的激动剂活性（半数有效浓度[EC50]值：141 nM），其最大效应与激动剂5-CT（EC50值：0.91 nM）相当，这与明显无活性的拮抗剂酮色林（平衡解离常数[KB]值：34 nM）不同。
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