PMID: 8947919Nov 1, 1996Paper

Sensitivity of opioid receptor binding to N-substituted maleimides and methanethiosulfonate derivatives

Neurochemical Research
M Shahrestanifar, Richard D Howells

Abstract

A series of N-substituted maleimides was shown to effectively inactivate bremazocine binding to delta opioid receptors. Apparent second order rate constants for inactivation increased with increasing size of the N-substituent: N-methyl < N-ethyl < N-butyl < N-phenylmaleimide. It is suggested that the positive chain length effect is attributed to nonpolar interactions with the receptor in the vicinity of the reactive group. Binding to mu and delta opioid receptors was equally sensitive to inactivation by (2-aminoethyl)methanethiosulfonate; the [2-(trimethylammonium)ethyl] and (2-sulfonatoethyl) derivatives were less active. Site-directed mutagenesis of the mu opioid receptor indicated that Cys159, Cys190, Cys235, Cys292, or Cys321, residing in transmembrane domain 3, 4, 5, 6, and 7, respectively, were not the site of modification.

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Citations

Aug 7, 2002·European Journal of Pharmacology·Faika MseehMargarita I Dubocovich
Oct 19, 2000·Brain Research. Molecular Brain Research·K ChaturvediR D Howells
Mar 17, 2000·Brain Research. Molecular Brain Research·K ChaturvediR D Howells
Jan 23, 2009·The Journal of Biological Chemistry·Ahmad B MaaroufShaohu Sheng
Mar 11, 2009·Frontiers in Bioscience (Landmark Edition)·Craig W Stevens
Feb 15, 2001·Biopolymers·K ChaturvediR D Howells
Jan 12, 2001·The Journal of Biological Chemistry·K ChaturvediR D Howells

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