舒马曲坦（GR43175）抑制犬离体隐静脉中环磷酸腺苷的积累。
Sumatriptan (GR43175) inhibits cyclic-AMP accumulation in dog isolated saphenous vein.
作者信息
Sumner M J, Humphrey P P
机构信息
Pharmacology Division, Glaxo Group Research Ltd., Ware, Hertfordshire.
出版信息
Br J Pharmacol. 1990 Feb;99(2):219-20. doi: 10.1111/j.1476-5381.1990.tb14682.x.
Abstract
Sumatriptan (GR43175) contracts rings of dog isolated saphenous vein by an action at 5-HT1-like receptors. We have now examined the effects of sumatriptan on prostaglandin E2(PGE2)-stimulated adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation in this tissue. Sumatriptan and 5-hydroxytryptamine (5-HT) produced a concentration-dependent inhibition of PGE2-stimulated cyclic AMP accumulation (EC50 values of 250 nM and 80 nM respectively), responses that were mimicked by 5-carboxamidotryptamine but not by U-46619 or methoxamine. The response to sumatriptan (1 microM) was antagonised by methiothepin (1 microM), but not by metergoline (0.1 microM), spiperone (1 microM) or ondansetron (GR38032, 1 microM). These results suggest that 5-HT1-like receptors which mediate contraction of the dog isolated saphenous vein are negatively coupled to adenylate cyclase in this preparation.
摘要
舒马曲坦（GR43175）通过作用于5-羟色胺1样受体使犬离体隐静脉环收缩。我们现在研究了舒马曲坦对该组织中前列腺素E2（PGE2）刺激的腺苷3':5'-环磷酸（环磷酸腺苷）积累的影响。舒马曲坦和5-羟色胺（5-HT）对PGE2刺激的环磷酸腺苷积累产生浓度依赖性抑制（EC50值分别为250 nM和80 nM），5-羧酰胺色胺可模拟该反应，但U-46619或甲氧明不能模拟。舒马曲坦（1 μM）的反应被甲硫噻平（1 μM）拮抗，但不被麦角苄酯（0.1 μM）、螺哌隆（1 μM）或昂丹司琼（GR38032，1 μM）拮抗。这些结果表明，介导犬离体隐静脉收缩的5-羟色胺1样受体在此制剂中与腺苷酸环化酶负偶联。
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Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus.对5-HT1A结合位点具有亲和力的中枢性降压药可抑制小牛海马体中福斯高林刺激的腺苷酸环化酶活性。
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