Antagonistic properties of [Phe3,Leu13]porcine motilin

European Journal of Pharmacology
I DepoortereT L Peeters

Abstract

We describe the antagonistic properties due to the replacement of Pro3 by phenylalanine in porcine motilin. The analogue, [Phe3,Leu13] porcine motilin (OHM-11526), displaces iodinated [Nle13]porcine motilin bound to a homogenate of rabbit antral smooth muscle tissue. The dissociation constant (pKd) was 9.26 +/- 0.04, versus 9.11 +/- 0.01 for motilin and 8.24 +/- 0.06 for ANQ-11125, the (1-14) fragment of OHM-11526. The Hill coefficient was close to one and Schild plot analysis confirmed the competitive nature of the interaction. In the tissue bath OHM-11526 was unable to induce contractions of segments of rabbit duodenum. At a concentration of 10(-6) M, OHM-11526 was unable to induce contractions of segments of rabbit duodenum. At a concentration of 10(-6) M, OHM-11526 inhibited the effect of maximally effective doses of porcine motilin and of the erythromycin derivative, EM-523, but was without effect on contractions induced by acetylcholine, substance P and serotonin. Increasing doses of OHM-11526 shifted the dose-response curves of motilin and EM-523 to the right, but caused a depression of the maximal response as well. From the motilin curves, and assuming a dual competitive and non-competitive interaction, the pA2 was 7.79...Continue Reading

References

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Citations

Mar 19, 1999·Clinical and Experimental Pharmacology & Physiology·M J ClarkJ B Furness
Feb 24, 2001·Chemical & Pharmaceutical Bulletin·M HaramuraE Murayama
Feb 13, 2001·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·G Van AsscheT L Peeters
Apr 12, 2016·Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology·Amrita DudaniTakafumi Sakai
May 12, 2009·Pharmacology & Therapeutics·Betty De SmetInge Depoortere
Mar 18, 2004·British Journal of Clinical Pharmacology·Ingrid M C KamerlingAd A M Masclee
Jan 25, 2000·American Journal of Physiology. Gastrointestinal and Liver Physiology·P MillerP Poitras
Jan 25, 2002·Journal of Medicinal Chemistry·Masayuki HaramuraEigoro Murayama

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