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5-羟色胺受体激动剂对福斯高林刺激的腺苷酸环化酶活性的抑制作用。

Inhibition of forskolin-stimulated adenylate cyclase activity by 5-HT receptor agonists.

作者信息

Devivo M, Maayani S

出版信息

Eur J Pharmacol. 1985 Dec 17;119(3):231-4. doi: 10.1016/0014-2999(85)90300-0.

Abstract

We measured the inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig hippocampal membranes by 5-HT, 5-carboxamidotryptamine (CAT) and 8-hydroxy-2-(di-n-propylamino) tetralin (PAT). Low concentrations of these agonists inhibited forskolin-stimulated adenylate cyclase activity in a concentration-dependent and saturable manner. The antagonist spiperone shifted the concentration-response curve to CAT to the right in a parallel manner. The EC50 values of CAT, PAT and 5-HT and the KB of spiperone suggest that this receptor may correspond to the 5-HT1A binding site.

摘要

我们测定了5-羟色胺(5-HT)、5-羧基酰胺色胺(CAT)和8-羟基-2-(二正丙基氨基)四氢萘(PAT)对豚鼠海马膜中福斯高林刺激的腺苷酸环化酶活性的抑制作用。这些激动剂的低浓度以浓度依赖性和饱和性方式抑制福斯高林刺激的腺苷酸环化酶活性。拮抗剂螺哌隆使CAT的浓度-反应曲线平行右移。CAT、PAT和5-HT的半数有效浓度(EC50)值以及螺哌隆的平衡解离常数(KB)表明,该受体可能对应于5-HT1A结合位点。

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