Literature DB >> 11078198

N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.

A Coop1, A E Jacobson, M D Aceto, L S Harris, J R Traynor, J H Woods, K C Rice.   

Abstract

The position of the indole in the indolomorphinans, which includes the delta opioid antagonist naltrindole, is considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be mu preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands.

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Year:  2000        PMID: 11078198     DOI: 10.1016/s0960-894x(00)00479-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  5'-halogenated analogs of oxymorphindole.

Authors:  Matthew D Metcalf; Andrew Coop
Journal:  Bioorg Med Chem Lett       Date:  2007-08-23       Impact factor: 2.823

2.  Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).

Authors:  Gianfranco Balboni; Remo Guerrini; Severo Salvadori; Lucia Negri; Elisa Giannini; Sharon D Bryant; Yunden Jinsmaa; Lawrence H Lazarus
Journal:  J Med Chem       Date:  2005-12-29       Impact factor: 7.446

  2 in total

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