Kalkman H O, Boddeke H W, Timmermans P B, Van Zwieten P A
J Auton Pharmacol. 1983 Dec;3(4):281-6. doi: 10.1111/j.1474-8673.1983.tb00546.x.
The pressor responses to six selective 5-HT receptor agonists, quipazine, TMFPP, Org 10155, Ru 24969, 5-methoxytryptamine and 5-methoxy-N,N-dimethyltryptamine, were quantified and tested for calcium dependency following i.v. administration to pithed normotensive rats. The pressor responses induced by 5-methoxytryptamine and 5-methoxy-N,N-dimethyltryptamine were not influenced by calcium entry blockade by means of nifedipine. The piperazine derivatives quipazine, TMFPP and Org 10155 were full agonists, but the pressor responses to these agonists were sensitive to calcium entry blockade. 5-Methoxy-N,N-dimethyltryptamine and Ru 24969 were found to be partial agonists. It is submitted as a hypothesis that within the present series of 5-HT receptor agonists, a restricted side chain flexibility will enhance the dependency of their pressor responses to extracellular calcium.
对六种种选择性5-羟色胺(5-HT)受体激动剂——喹哌嗪、TMFPP、Org 10155、Ru 24969、5-甲氧基色胺和5-甲氧基-N,N-二甲基色胺的升压反应进行了定量,并在给脊髓切断的正常血压大鼠静脉注射后测试其钙依赖性。5-甲氧基色胺和5-甲氧基-N,N-二甲基色胺诱导的升压反应不受硝苯地平对钙内流的阻断影响。哌嗪衍生物喹哌嗪、TMFPP和Org 10155是完全激动剂,但这些激动剂的升压反应对钙内流阻断敏感。5-甲氧基-N,N-二甲基色胺和Ru 24969被发现是部分激动剂。作为一种假设提出,在本系列5-HT受体激动剂中,有限的侧链柔韧性将增强其升压反应对细胞外钙的依赖性。