Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.

Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
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α-肾上腺素受体试剂。

DOI:
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发表时间:
1986
影响因子:
7.3
通讯作者:
I. Tulloch
I. Tulloch
中科院分区:
医学1区
文献类型:
--
作者:
A. P. Welbourn;C. Chapleo;A. C. Lane;P. Myers;A. Roach;C. Smith;M. Stillings;I. Tulloch

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本文报道了三种咪唑克生2-取代衍生物的拆分。对映异构体在各种体外和体内试验中显示出大的活性分离,并且活性异构体都是α 2-肾上腺素受体的有效和选择性拮抗剂。这些结果的意义有关的对映异构体的咪唑克生和光学活性α 2-肾上腺素受体激动剂发表了讨论。
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.