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Abstract

EFFECTS OF NEWLY SYNTHESIZED ENDOMORPHIN-2 ANALOGS ON GUINEA PIG ILEUM

Kaloyan Georgiev*, Boris Kadinov and Tamara Pajpanova

ABSTRACT

Endomorphin-1and endomorphin-2 are opioid tetrapeptides, which are
isolated from bovine and human brain and have high affinity and
selectivity to central μ-opioid receptors. In the digestive tract, opioidlike
drugs inhibit peristalsis and induce constipation. In this study, we
analyzed the effects of newly synthesized endomorphin-2 analogs –
Deoxycholic-Tyr-Pro-Phe(pCl)-Phe-OH and Deoxycholic-Tyr-Pro-
Phe(pF)-Phe-OH, on longitudinal muscle preparations from the guineapig
ileum (GPI). The both analogs used alone slightly affect
spontaneous contractility of longitudinal muscle, but they significantly
reduce acetylcholine-induced contractility. The use of μ-opioid
receptor antagonist – naloxone increase the inhibitory effects on
acetylcholine-stimulated contractility of GPI. Further research is
necessary to explain this interaction.

Keywords: endomorphin, nociception, ?-opioid receptor, deoxycholic acid, unnatural amino acids, naloxone.


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