BMY 7378是α1肾上腺素能受体D亚型的选择性拮抗剂。
BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors.
作者信息
Goetz A S, King H K, Ward S D, True T A, Rimele T J, Saussy D L
机构信息
Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.
出版信息
Eur J Pharmacol. 1995 Jan 16;272(2-3):R5-6. doi: 10.1016/0014-2999(94)00751-r.
BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8- azaspiro[4.5]decane-7,9-dione dihydrochloride), a 5-HT1A receptor partial agonist, also binds to alpha 1-adrenoceptors. Competition assays were performed using (+/-)-beta-([125I]iodo-4-hydroxyphenyl)-ethyl-aminomethyl-tetralone ([125I]HEAT), and membranes prepared from Rat-1 fibroblasts expressing hamster alpha 1b-, bovine alpha 1c-, or rat alpha 1d-adrenoceptor, or their respective human homologues. Results indicate that BMY 7378 is selective for the alpha 1D-adrenoceptor subtype (pKi: hamster alpha 1b-adrenoceptor 6.2 +/- 0.03, human alpha 1b-adrenoceptor 7.2 +/- 0.05; bovine alpha 1c-adrenoceptor 6.1 +/- 0.02, human alpha 1c-adrenoceptor 6.6 +/- 0.20; rat alpha 1d-adrenoceptor 8.2 +/- 0.06, human alpha 1d-adrenoceptor 9.4 +/- 0.05) and has high affinity (pA2, 8.9 +/- 0.1) for rat aorta alpha 1-adrenoceptor.
BMY 7378（8-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-8-氮杂螺[4.5]癸烷-7,9-二酮二盐酸盐），一种5-HT1A受体部分激动剂，也能与α1-肾上腺素能受体结合。使用(+/-)-β-([125I]碘-4-羟基苯基)-乙基-氨基甲基四氢萘酮([125I]HEAT)以及由表达仓鼠α1b-、牛α1c-或大鼠α1d-肾上腺素能受体或其各自人类同源物的大鼠-1成纤维细胞制备的膜进行竞争试验。结果表明，BMY 7378对α1D-肾上腺素能受体亚型具有选择性（pKi：仓鼠α1b-肾上腺素能受体6.2±0.03，人类α1b-肾上腺素能受体7.2±0.05；牛α1c-肾上腺素能受体6.1±0.02，人类α1c-肾上腺素能受体6.6±0.20；大鼠α1d-肾上腺素能受体8.2±0.06，人类α1d-肾上腺素能受体9.4±0.05），并且对大鼠主动脉α1-肾上腺素能受体具有高亲和力（pA2，8.9±0.1）。
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