N-cyclohexylethyl-N-noroxymorphindole: A mu-opioid preferring analogue of naltrindole

The position of the indole in the indolomorphinans, which includes the delt a opioid antagonist naltrindole, is considered to be responsible for the de lta opioid selectivity for this class of ligands. Herein is described the N -cyclohexylethyl substituted N-nor-derivative, which is shown to be mu pref erring. Thus, the nature of the N-substituent is equally important to the r eceptor selectivity for this class of ligands. (C) 2000 Elsevier Science Lt d. All rights reserved.