Differential discrimination of G-protein coupling of serotonin1A receptors from bovine hippocampus by an agonist and an antagonist

被引:43
作者
Harikumar, KG [1 ]
Chattopadhyay, A [1 ]
机构
[1] Ctr Cellular & Mol Biol, Hyderabad 500007, Andhra Pradesh, India
关键词
5-hydroxytryptamine(1A) receptor; 8-hydroxy-2-(di-N-propylamino)tetralin; 4-(2 '-methoxy)-pheny-1-1-(2 '-(N-2 ''-pyridinyl)-p-fluorobenzamido)ethyl-piperazine; G-protein coupling; guanosine-5 '-O-(3-thiotriphosphate); bovine hippocampus;
D O I
10.1016/S0014-5793(99)01082-0
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have studied the effect of guanosine-5'-O-(3-thiotriphosphate) (GTP-gamma-S), a non-hydrolyzable analogue of GTP, on agonist and antagonist binding to bovine hippocampal 5-hydroxytryptamine (5-HT)(1A) receptor in native membranes. Our results show that the specific binding of the agonist is inhibited with increasing concentrations of GTP-gamma-S along with a reduction in binding affinity. In sharp contrast to this, antagonist binding to 5-HT1A receptor shows no significant reduction and remains invariant over a large range of GTP-gamma-S concentrations, The binding affinity of the antagonist also remains unaltered. This shows that the agonist and the antagonist differentially discriminate G-protein coupling of 5-HT1A receptors from bovine hippocampus. (C) 1999 Federation of European Biochemical Societies.
引用
收藏
页码:389 / 392
页数:4
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