介导人隐静脉收缩的α2 -肾上腺素能受体亚型的研究。
Investigations of the subtype of alpha 2-adrenoceptor mediating contractions of the human saphenous vein.
作者信息
Smith K, Connaughton S, Docherty J R
机构信息
Department of Clinical Pharmacology, Royal College of Surgeons in Ireland, Dublin.
出版信息
Br J Pharmacol. 1992 Jun;106(2):447-51. doi: 10.1111/j.1476-5381.1992.tb14354.x.
Abstract
- We have examined the effects of a series of alpha 2-adrenoceptor antagonists against isometric contractions to noradrenaline in human saphenous vein, and correlated these potencies with affinities for the alpha 2A-ligand binding site of human platelet and the alpha 2B-ligand binding site of rat kidney. 2. The alpha 2B-selective adrenoceptor antagonists, prazosin, ARC 239 and HV 723 showed high, and the alpha 2A-selective antagonist BRL 44408 showed low, potency in human saphenous vein. 3. Potency in human saphenous vein correlated better with affinity for the alpha 2B-ligand binding site (r = 0.71, n = 12, P less than 0.01) than with affinity for the alpha 2A-ligand binding site (r = 0.56, n = 12, non significant). 4. It is concluded that the postjunctional alpha 2-adrenoceptor of human saphenous vein resembles an alpha 2B-ligand binding site more than an alpha 2A-ligand binding site.
摘要
- 我们研究了一系列α2-肾上腺素能受体拮抗剂对人隐静脉中去甲肾上腺素等长收缩的影响，并将这些效能与对人血小板α2A-配体结合位点及大鼠肾脏α2B-配体结合位点的亲和力进行了关联。2. α2B选择性肾上腺素能受体拮抗剂哌唑嗪、ARC 239和HV 723在人隐静脉中显示出高效能，而α2A选择性拮抗剂BRL 44408则显示出低效能。3. 人隐静脉中的效能与对α2B-配体结合位点的亲和力（r = 0.71，n = 12，P < 0.01）的相关性优于与对α2A-配体结合位点的亲和力（r = 0.56，n = 12，无显著性）。4. 得出的结论是，人隐静脉的节后α2-肾上腺素能受体更类似于α2B-配体结合位点而非α2A-配体结合位点。
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本文引用的文献
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Postsynaptic alpha-adrenoceptor subtypes in rabbit blood vessels and rat anococcygeus muscle studied in vitro.体外研究兔血管和大鼠肛尾肌中的突触后α-肾上腺素能受体亚型。
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