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(R)-和(S)-盐酸羟苯环胺的抗毒蕈碱作用

Antimuscarinic effects of (R)- and (S)- oxyphencyclimine hydrochloride.

作者信息

Schjelderup L, Kozlowski M R, Weissman A, Aasen A J

机构信息

Department of Chemistry, Agricultural University of Norway.

出版信息

Pharm Res. 1988 Apr;5(4):236-7. doi: 10.1023/a:1015945830309.

Abstract

The (R)-(+)- and (S)-(-)-enantiomers of the anticholinergic compound, oxyphencyclimine, were synthesized from (R)-(-)- and (S)-(+)-2-cyclohexyl-2-hydroxy-2-phenylethanoic acid, respectively. The potencies of the enantiomers were compared using a cholinergic receptor binding assay. The (R)-(+)-enantiomer inhibited binding 29 times more potently than the (S)-(-)-enantiomer.

摘要

抗胆碱化合物羟苯环壬酯的(R)-(+)-和(S)-(-)-对映体分别由(R)-(-)-和(S)-(+)-2-环己基-2-羟基-2-苯乙酸合成。使用胆碱能受体结合试验比较了对映体的效力。(R)-(+)-对映体抑制结合的效力比(S)-(-)-对映体强29倍。

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