PMID: 9416781Jan 1, 1997Paper

Tyr1]-nociceptin has naloxone-insensitive vasodilator activity in the hindquarters vascular bed of the rat

Life Sciences
H C Champion, P J Kadowitz

Abstract

The heptadecapeptide nociceptin, also known as Orphanin FQ, is a newly-discovered endogenous ligand for the opioid-like G-protein-coupled receptor ORL1. In the present study, in order to investigate the structure-activity relationship for nociceptin, responses to nociceptin, [Tyr1]-nociceptin, nociceptin-(2-17), nociceptin-(1-11), and nociceptin-(1-7) were compared in the hindquarters vascular bed of the rat. Injections of nociceptin (1-30 nmol), [Tyr1]-nociceptin (1-30 nmol), and met-enkephalin (10-300 nmol) induced dose-related decreases in hindquarters perfusion pressure, whereas injections of similar volumes of the saline vehicle had no effect. In terms of relative vasodilator activity, [Tyr1]-nociceptin was similar to nociceptin, and these peptides were approximately 10-fold more potent than met-enkephalin in decreasing hindquarters perfusion pressure. In contrast, nociceptin-(2-17), nociceptin-(1-11), and nociceptin-(1-7) had no significant effect on hindquarters perfusion pressure when injected into the perfusion circuit in doses up to 100 nmol. The decreases in hindquarters perfusion pressure in response to [Tyr1]-nociceptin and nociceptin were not altered by the opioid receptor antagonist naloxone at a time when respon...Continue Reading

References

Jun 14, 1996·The Journal of Biological Chemistry·R K ReinscheidO Civelli
Aug 6, 1996·Proceedings of the National Academy of Sciences of the United States of America·C MollereauM Parmentier
Aug 6, 1996·Proceedings of the National Academy of Sciences of the United States of America·H P NothackerO Civelli

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