Postjunctionalα肾上腺素受体(2 c)在人类隐静脉收缩性。

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Rizzo CA、皱LM Corboz先生,Umland SP, Wan Y,沙H, Jakway J,程L,麦考密克K,伊根RW,嘿农协

Postjunctionalα肾上腺素受体(2 c)在人类隐静脉收缩性。

欧元J杂志。2001年2月16日,413 (2):263 - 9。

PubMed ID

11226402 (在PubMed

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文摘

postjunctionalα(2)-adrenoceptor-mediated收缩性特点是在人类隐静脉来自冠状动脉搭桥手术。人类隐静脉收缩α(2)肾上腺素能受体选择性受体激动剂二叔丁基对甲酚- 920 (5、6、7,8-Tetrahydro-6——(2-propenyl) 4 h-thiazolo [4, 5 d] azepin-2-amine盐酸盐;pD(2) = 6.7 + / - -0.1)和英国14304 (5-Bromo-6——(2-imidazolin-2-ylamino)喹喔啉;pD (2) = 7.2 + / - -0.1)。二叔丁基对甲酚- 920诱导宫缩抑制α(2)肾上腺素能受体拮抗剂育亨宾(17-Hydroxy-yohimban-16-carboxylic酸甲酯盐酸盐;pA(2) = 8.7 + / - -0.5),但不是由α(1)肾上腺素能受体拮抗剂哌唑嗪(1 - [4-Amino-6 7-dimethoxy-2-quinazolinyl] 4 - [2-furanylcarbonyl]哌嗪盐酸盐;300海里)。相比之下,哌唑嗪(pK (b) = 7.9 + / - -0.2)引起强有力地收缩引起的α(1)肾上腺素能受体激动剂苯肾上腺素((R) 3-hydroxy-alpha - [(methylamino)甲基]大盐酸盐;pD(2) = 4.9 + / - -0.1),表明这两个α(2)- - -α(1)肾上腺素能受体唤起人类隐静脉收缩。功能拮抗剂活动估计(pA(2)或pK (b))获得239年alpha-adrenoceptor拮抗剂弧(2 - [2 - (4 - (2-Methoxyphenyl) piperazin-1-yl)乙基]4,4-dimethyl-1, 3 - (2 h, 4 h) -isoquino lindione盐酸盐),世行4101 (2 - (2,6-Dimethoxyphenoxyethyl) aminomethyl-1 4-benzodioxane盐酸)和高压723 (alpha-ethyl-3 4 5-trimethoxy-alpha - (3 - ((2 - (2-methoxyphenoxy)乙基)氨基)丙基)benzeneacetonitrile)和二叔丁基对甲酚- 920诱导人类隐静脉收缩是7.0 + / - -0.6,8.3 + / - -0.6和7.7 + / - -0.3,分别。 The alpha(2)-adrenoceptor subtype affinities (pK(i)) obtained in recombinant human alpha(2A)-, alpha(2B)- and alpha(2C)-adrenoceptor competition binding assays were 8.6, 8.3 and 8.6 for yohimbine; 6.3, 8.4 and 7.0 for ARC 239; 8.4, 7.5 and 8.4 for WB 4101 and 7.5, 7.4 and 7.9 for HV 723, respectively. Taken together, the binding and functional antagonist activity estimates obtained in these investigations indicate that alpha(2C)-adrenoceptor is the predominant postjunctional alpha(2)-adrenoceptor subtype in human saphenous vein.

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药物靶点

药物	目标	类	生物	药理作用	行动
育亨宾	Alpha-2C肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节