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Title: FMRFamide: low affinity inhibition of opioid binding to rabbit brain membranes

Abstract

FMRFamide (Phe-Met-Arg-Phe-NH/sub 2/) was first isolated from the ganglia of molluscs by Price and Greenberg in 1977. The peptide was subsequently shown to have diverse actions on various types of molluscan and mammalian tissues. The presence of immunoreactive FMRFamide-like material (irFMRF) in multiple areas of rat brain, spinal cord, and gastrointestinal tract suggests that irFMRF may have a physiological role in mammals. Tang, Yang and Costa recently demonstrated that FMRFamide attenuates morphine antinociception in rats and postulated, based on this and several other lines of evidence, that irFMRF might be an endogenous opioid antagonist. In the present study, they tested the ability of FMRFamide to inhibit the binding of opioid receptor ligands to rabbit membrane preparations. FMRFamide inhibited the specific binding of both /sup 3/(H)-dihydromorphine and /sup 3/(H)-ethylketocyclazocine (IC/sub 50/ = 14 ..mu..M and 320 ..mu..M, respectively) in a dose-related manner, suggesting that FMRFamide may affect binding to at least two types of opioid receptors (mu and kappa). These data are consistent with the concept that irFMRF might act as an endogenous opioid antagonist. However, the low affinity of FMRFamide leaves open the possibility of another mechanism of opioid antagonism, such as neuromodulation.

Authors:
;
Publication Date:
Research Org.:
Temple Univ. School of Medicine, Philadelphia, PA
OSTI Identifier:
7119570
Report Number(s):
CONF-8604222-
Journal ID: CODEN: FEPRA; TRN: 87-007013
Resource Type:
Conference
Journal Name:
Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)
Additional Journal Information:
Journal Volume: 45:4; Conference: 70. annual meeting of the Federation of American Society for Experimental Biology, St. Louis, MO, USA, 13 Apr 1986
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; MORPHINE; RECEPTORS; PEPTIDES; BIOLOGICAL EFFECTS; BIOCHEMICAL REACTION KINETICS; AMIDES; BRAIN; CELL MEMBRANES; DOSE-RESPONSE RELATIONSHIPS; IMMUNE REACTIONS; INHIBITION; LIGANDS; RABBITS; TRACER TECHNIQUES; TRITIUM COMPOUNDS; ALKALOIDS; ANALGESICS; ANIMALS; BODY; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM DEPRESSANTS; DRUGS; ISOTOPE APPLICATIONS; KINETICS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; NARCOTICS; NERVOUS SYSTEM; OPIUM; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANS; PROTEINS; REACTION KINETICS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Zhu, X Z, and Raffa, R B. FMRFamide: low affinity inhibition of opioid binding to rabbit brain membranes. United States: N. p., 1986. Web.
Zhu, X Z, & Raffa, R B. FMRFamide: low affinity inhibition of opioid binding to rabbit brain membranes. United States.
Zhu, X Z, and Raffa, R B. 1986. "FMRFamide: low affinity inhibition of opioid binding to rabbit brain membranes". United States.
@article{osti_7119570,
title = {FMRFamide: low affinity inhibition of opioid binding to rabbit brain membranes},
author = {Zhu, X Z and Raffa, R B},
abstractNote = {FMRFamide (Phe-Met-Arg-Phe-NH/sub 2/) was first isolated from the ganglia of molluscs by Price and Greenberg in 1977. The peptide was subsequently shown to have diverse actions on various types of molluscan and mammalian tissues. The presence of immunoreactive FMRFamide-like material (irFMRF) in multiple areas of rat brain, spinal cord, and gastrointestinal tract suggests that irFMRF may have a physiological role in mammals. Tang, Yang and Costa recently demonstrated that FMRFamide attenuates morphine antinociception in rats and postulated, based on this and several other lines of evidence, that irFMRF might be an endogenous opioid antagonist. In the present study, they tested the ability of FMRFamide to inhibit the binding of opioid receptor ligands to rabbit membrane preparations. FMRFamide inhibited the specific binding of both /sup 3/(H)-dihydromorphine and /sup 3/(H)-ethylketocyclazocine (IC/sub 50/ = 14 ..mu..M and 320 ..mu..M, respectively) in a dose-related manner, suggesting that FMRFamide may affect binding to at least two types of opioid receptors (mu and kappa). These data are consistent with the concept that irFMRF might act as an endogenous opioid antagonist. However, the low affinity of FMRFamide leaves open the possibility of another mechanism of opioid antagonism, such as neuromodulation.},
doi = {},
url = {https://www.osti.gov/biblio/7119570}, journal = {Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)},
number = ,
volume = 45:4,
place = {United States},
year = {Wed Mar 05 00:00:00 EST 1986},
month = {Wed Mar 05 00:00:00 EST 1986}
}

Conference:
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