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Identification and exploitation of the. sigma.-opiate pharmacophore

…, AM Ismaiel, M El-Ashmawy, G Battaglia…

文献索引:Glennon, Richard A.; Smith, J. Doyle; Ismaiel, Abd M.; El-Ashmawy, Mahmoud; Battaglia, George; Fisher, James B. Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1094 - 1098

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被引用次数: 32

摘要

Certain benzomorphan" u-opiates" such as N-allylnormetazocine (NANM) bind at u receptors with modest affinity and with little selectivity (ie, they also bind at phencyclidine or PCP sites). In order to identify the primary pharmacophore of the benzomorphans, we prepared several aminesubtituted derivatives of 1-phenyl-2-aminopropane. Several simple alkyl-substituted analogues were shown to bind at u sites with affinities comparable to that ...