Document Detail


Endomorphin 1 and 2, endogenous mu-opioid agonists, decrease systemic arterial pressure in the rat.
MedLine Citation:
PMID:  9519803     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The endogenous opioid peptides, endomorphin 1 and 2, are newly isolated, potent, and selective mu-opioid receptor agonists. In the present study, responses to endomorphin 1 and 2 were investigated in the systemic vascular bed of the rat. Endomorphin 1 and 2 induced dose-related decreases in systemic arterial pressure when injected in doses of 1-30 nmol/kg i.v. In terms of relative vasodepressor activity, endomorphin 1 and 2 were approximately equipotent with each other and with the ORL1 ligand, nociceptin (orphanin FQ), and were about 10-fold more potent than met-enkephalin in decreasing systemic arterial pressure. Vasodepressor responses to endomorphin 1 and 2 and met-enkephalin, but not to nociceptin, were inhibited by the opioid receptor antagonist, naloxone. These results demonstrate that endomorphin 1 and 2 produce significant naloxone-sensitive decreases in systemic arterial pressure.
Authors:
M A Czapla; H C Champion; J E Zadina; A J Kastin; L Hackler; L J Ge; P J Kadowitz
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Life sciences     Volume:  62     ISSN:  0024-3205     ISO Abbreviation:  Life Sci.     Publication Date:  1998  
Date Detail:
Created Date:  1998-04-06     Completed Date:  1998-04-06     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  0375521     Medline TA:  Life Sci     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  PL175-9     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Tulane University School of Medicine, New Orleans, Louisiana 70112, USA.
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MeSH Terms
Descriptor/Qualifier:
Analgesics, Opioid / pharmacokinetics,  pharmacology*
Animals
Blood Pressure / drug effects*
Enkephalin, Methionine / pharmacology
Female
Male
Oligopeptides / pharmacokinetics,  pharmacology*
Opioid Peptides / pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Opioid, mu / agonists*
Vasoconstrictor Agents / pharmacokinetics,  pharmacology*
Chemical
Reg. No./Substance:
0/Analgesics, Opioid; 0/Oligopeptides; 0/Opioid Peptides; 0/Receptors, Opioid, mu; 0/Vasoconstrictor Agents; 0/endomorphin 1; 0/endomorphin 2; 0/nociceptin; 58569-55-4/Enkephalin, Methionine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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