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毒蕈碱对大鼠阴茎前列环素合成的刺激作用。

Muscarinic stimulation of prostacyclin synthesis by the rat penis.

作者信息

Jeremy J Y, Mikhailidis D P, Dandona P

出版信息

Eur J Pharmacol. 1986 Apr 9;123(1):67-71. doi: 10.1016/0014-2999(86)90688-6.

Abstract

An in vitro model for the investigation of PGI2 synthesis by the rat penis is described. Acetyl-beta-methylcholine (methacholine; MeCh) and carbamyl choline (carbachol) stimulated PGI2 synthesis in a dose-dependent manner (ED50 = 1.5 X 10(-6); 2.5 X 10(-6), respectively), whereas adrenaline, noradrenaline, histamine, serotonin, vasoactive intestinal polypeptide (VIP), nicotine, dimethyl phenylpiperazinium (DMPP) and adenosine triphosphate (ATP) were without effect. MeCh (10(-6) mol/l)- and carbachol (10(-6) mol/l)-stimulated PGI2 synthesis was inhibited by atropine in a dose-dependent manner (ID50 = 2.5 X 10(-7) mol/l; 7 X 10(-6) mol/l, respectively). The inhibition by atropine of MeCh-stimulated PGI2 synthesis was competitive. MeCh (10(-6) mol/l)-stimulated PGI2 synthesis was inhibited by verapamil (ID50 = 6 X 10(-5)) and calcium-free incubation media. It is concluded that in the rat penis PGI2 synthesis is principally under muscarinic control and is calcium transport-dependent. Since PGI2 is a vasodilator, these findings may be relevant to the increased blood flow into the penis associated with penile erection. They may also be relevant to the protection of the penile vasculature from thrombosis, since PGI2 is also a potent inhibitor of platelet aggregation.

摘要

本文描述了一种用于研究大鼠阴茎合成前列环素(PGI2)的体外模型。乙酰-β-甲基胆碱(醋甲胆碱;MeCh)和氨甲酰胆碱刺激PGI2合成呈剂量依赖性(ED50分别为1.5×10^(-6);2.5×10^(-6)),而肾上腺素、去甲肾上腺素、组胺、5-羟色胺、血管活性肠肽(VIP)、尼古丁、二甲基苯基哌嗪(DMPP)和三磷酸腺苷(ATP)则无作用。MeCh(10^(-6)mol/L)和氨甲酰胆碱(10^(-6)mol/L)刺激的PGI2合成被阿托品以剂量依赖性方式抑制(ID50分别为2.5×10^(-7)mol/L;7×10^(-6)mol/L)。阿托品对MeCh刺激的PGI2合成的抑制作用是竞争性的。MeCh(10^(-6)mol/L)刺激的PGI2合成被维拉帕米(ID50 = 6×10^(-5))和无钙孵育培养基抑制。得出的结论是,在大鼠阴茎中,PGI2合成主要受毒蕈碱控制且依赖钙转运。由于PGI2是一种血管舒张剂,这些发现可能与阴茎勃起时阴茎血流量增加有关。它们也可能与保护阴茎血管系统免受血栓形成有关,因为PGI2也是血小板聚集的有效抑制剂。

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