α-肾上腺素能受体试剂。4. 一些强效选择性突触前α2-肾上腺素能受体拮抗剂的拆分。
Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
作者信息
Welbourn A P, Chapleo C B, Lane A C, Myers P L, Roach A G, Smith C F, Stillings M R, Tulloch I F
出版信息
J Med Chem. 1986 Oct;29(10):2000-3. doi: 10.1021/jm00160a033.
PMID:2876101
Abstract
The resolution of three 2-substituted derivatives of idazoxan is described. The enantiomers show large separations in activity in a variety of in vitro and in vivo tests, and the active isomers are all potent and selective antagonists at the alpha 2-adrenoreceptor. The significance of these results in relation to those published on the enantiomers of idazoxan and to those on optically active alpha 2-adrenoreceptor agonists is discussed.
摘要
描述了伊达唑烷的三种2-取代衍生物的拆分情况。对映体在各种体外和体内试验中显示出活性上的巨大差异，且活性异构体均为强效且选择性的α2-肾上腺素能受体拮抗剂。讨论了这些结果与已发表的伊达唑烷对映体的结果以及与光学活性α2-肾上腺素能受体激动剂的结果相关的意义。
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