Identification and exploitation of the. sigma.-opiate pharmacophore

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

Index: 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

Full Text: HTML

Citation Number: 32

Abstract

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 ...