Literature DB >> 86208

Chloroxymorphamine, and opioid receptor site-directed alkylating agent having narcotic agonist activity.

T P Caruso, A E Takemori, D L Larson, P S Portoghese.   

Abstract

Chloroxymorphamine, the 6beta-N,N-bis(2-chloroethyl) derivative of oxymorphone, is a potent nonequilibrium narcotic agonist in the longitudinal muscle preparation of guinea pig ileum. The corresponding naltrexone analog,chlornaltrexamine, is a potent nonequilibrium antagonist of morphine. These receptor sitedirected alkylating agents possess considerable potenial as pharmacologic and biochemical probes of apoid receptors.

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Year:  1979        PMID： 86208     DOI： 10.1126/science.86208

Source DB:  PubMed          Journal:  Science        ISSN： 0036-8075            Impact factor:   47.728


  6 in total

1.  Pharmacological analysis of the calcium-dependence of mu-receptor agonism.

Authors:  I G Dougall; P Leff
Journal:  Br J Pharmacol       Date:  1987-12       Impact factor: 8.739

2.  Opioid receptor reserve in normal and morphine-tolerant guinea pig ileum myenteric plexus.

Authors:  C Chavkin; A Goldstein
Journal:  Proc Natl Acad Sci U S A       Date:  1984-11       Impact factor: 11.205

3.  Affinity labeling mu opioid receptors with novel radioligands.

Authors:  Ke Yang; Amy Zuckerman; Gavril W Pasternak
Journal:  Cell Mol Neurobiol       Date:  2005-06       Impact factor: 5.046

4.  Highly selective photoaffinity labeling of mu and delta opioid receptors.

Authors:  C Garbay-Jaureguiberry; A Robichon; V Daugé; P Rossignol; B P Roques
Journal:  Proc Natl Acad Sci U S A       Date:  1984-12       Impact factor: 11.205

5.  Estimation of opioid receptor agonist dissociation constants with beta-chlornaltrexamine, an irreversible ligand which also displays agonism.

Authors:  P Leff; I G Dougall
Journal:  Br J Pharmacol       Date:  1988-09       Impact factor: 8.739

6.  Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.

Authors:  Ákos Urai; András Váradi; Levente Szőcs; Balázs Komjáti; Valerie Le Rouzic; Amanda Hunkele; Gavril W Pasternak; Susruta Majumdar; Sándor Hosztafi
Journal:  Medchemcomm       Date:  2016-10-18       Impact factor: 3.597
  6 in total

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