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某些5-羟色胺1样受体激动剂对脊髓麻醉大鼠的血管突触后效应。

Vascular postsynaptic effects of some 5-HT1-like receptor agonists in the pithed rat.

作者信息

Dabiré H, Cherqui C, Fournier B, Schmitt H

机构信息

INSERM U228, Faculté de Médecine Broussais Hôtel-Dieu, Paris, France.

出版信息

Eur J Pharmacol. 1988 May 20;150(1-2):143-8. doi: 10.1016/0014-2999(88)90760-1.

Abstract

5-HT induced an increase in blood pressure in the pithed rat which was antagonized by LY 53857 a selective 5-HT2 receptor antagonist. It was not antagonized by spiroxatrine, MDL 72222, idazoxan or AR-C 239, respectively 5-HT1-like and 5-HT3 receptor antagonists, alpha 2- and alpha 1-adrenoceptor antagonists. 5-MeODMT also induced an increase in blood pressure which was antagonized by LY 53857 but not by the other 5-HT receptor antagonists and alpha-adrenoceptor antagonists used, suggesting a 5-HT2 component in the pressor effect of 5-MeODMT. The maximal effect of 5-MeODMT was less marked than that of 5-HT. 8-OH-DPAT, RU 24969 and TFMPP were far less effective than 5-HT and 5-MeODMT to increase blood pressure. In contrast, 5-CT induced a vasodepressor effect. It is therefore suggested that the vasoconstriction induced by 5-HT and by 5-MeODMT in pithed rats could be due mainly to the selective stimulation of postjunctional 5-HT2 receptors because selective alpha 1- and alpha 2-adrenoceptor antagonists were ineffective against the vasoconstrictor effects of 5-HT and 5-MeODMT. The relative lack of effect of 8-OH-DPAT, RU 24969 and TFMPP to increase blood pressure suggested that postjunctional 5-HT1-like receptors play only a minor role - if any - in 5-HT induced vasoconstriction in the pithed rat.

摘要

5-羟色胺(5-HT)可使脊髓切断大鼠的血压升高,这种作用可被选择性5-HT2受体拮抗剂LY 53857所拮抗。而分别作为5-HT1样和5-HT3受体拮抗剂、α2-和α1-肾上腺素能受体拮抗剂的螺沙群、MDL 72222、咪唑克生或AR-C 239对此并无拮抗作用。5-甲氧基-N,N-二甲基色胺(5-MeODMT)也可使血压升高,且同样被LY 53857所拮抗,但所用的其他5-HT受体拮抗剂和α-肾上腺素能受体拮抗剂对此并无拮抗作用,这表明5-MeODMT的升压作用中有5-HT2成分。5-MeODMT的最大效应不如5-HT明显。8-羟基二丙胺基四氢萘(8-OH-DPAT)、RU 24969和三氟甲基苯哌嗪(TFMPP)升高血压的作用远不如5-HT和5-MeODMT有效。相比之下,5-羧色胺(5-CT)可引起血管减压效应。因此,有人提出,5-HT和5-MeODMT在脊髓切断大鼠中所诱导的血管收缩可能主要是由于对节后5-HT2受体的选择性刺激,因为选择性α1-和α2-肾上腺素能受体拮抗剂对5-HT和5-MeODMT的血管收缩作用无效。8-OH-DPAT、RU 24969和TFMPP升高血压作用相对较弱,这表明节后5-HT1样受体在脊髓切断大鼠中5-HT诱导的血管收缩中即使有作用也只起次要作用。

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