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Endomorphin 1 and 2, endogenous mu-opioid agonists, decrease systemic arterial pressure in the rat

M A Czapla1, H C Champion, J E Zadina

  • 1Department of Pharmacology, Tulane University School of Medicine, New Orleans, Louisiana 70112, USA.

Life Sciences
|March 31, 1998
PubMed
Summary
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Newly discovered endomorphin 1 and 2 peptides significantly lower blood pressure in rats. These effects are mediated by mu-opioid receptors and are blocked by naloxone, confirming their opioid nature.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Cardiovascular Physiology

Background:

  • Endogenous opioid peptides play crucial roles in regulating physiological functions.
  • Endomorphin 1 and 2 are recently identified potent and selective agonists for the mu-opioid receptor.

Purpose of the Study:

  • To investigate the effects of endomorphin 1 and 2 on the systemic vascular bed in rats.
  • To characterize the vasodepressor activity and receptor mediation of endomorphin 1 and 2.

Main Methods:

  • Intravenous administration of endomorphin 1 and 2 in varying doses (1-30 nmol/kg) to rats.
  • Measurement of systemic arterial pressure changes.
  • Assessment of responses to opioid receptor antagonist naloxone and nociceptin.

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Main Results:

  • Endomorphin 1 and 2 induced dose-dependent reductions in systemic arterial pressure.
  • Endomorphin 1 and 2 exhibited equipotent vasodepressor activity, comparable to nociceptin and significantly greater than met-enkephalin.
  • Naloxone administration inhibited the vasodepressor effects of endomorphin 1 and 2, as well as met-enkephalin, but not nociceptin.

Conclusions:

  • Endomorphin 1 and 2 elicit significant, naloxone-sensitive decreases in systemic arterial pressure in rats.
  • These findings confirm the role of mu-opioid receptors in mediating the cardiovascular effects of endomorphins.