PMID: 7541284Apr 1, 1995Paper

Vascular actions of thrombin receptor-derived polypeptides: structure-activity profiles for contractile and relaxant effects in rat aorta

British Journal of Pharmacology
A Laniyonu, Morley D Hollenberg

Abstract

1. Using endothelium-denuded and intact rat aortic rings, we have determined the contractile and relaxant structure-activity profile for a series of thrombin receptor-derived polypeptides (TRPs) based on the human and rat receptor sequences: SFLLR (P5), SFLLR-NH2 (P5-NH2) SFFLR (Rat P5), SFFLR-NH2 (Rat P5-NH2), SFLLRNP (P7), SFLLRNP-NH2 (P7-NH2), SFFLRNP (Rat P7), SFFLRNP-NH2 (Rat P7-NH2), and SFLLRNPNDKYEPF (P14). 2. A contractile response to thrombin and the TRPs in the endothelium-denuded aortic tissue was minimal or absent in preparations obtained from animal weighing less than 180 g (< 6 weeks of age), but increased with animal size, plateauing in tissues derived from animals weighing between 320 and 420 g (about 9 to 14 weeks of age). In contrast, the contractile responses to KCl and noradrenaline did not differ in the tissues and relaxant responses to the TRPs in endothelium-intact aortic preparations were comparable for tissues obtained from either young (< or = 180 g) or older (> or = 320 g) animals. 3. The contractile response of the endothelium-denuded preparation to thrombin and the TRPs showed marked cross-desensitization: the relaxation response of the intact rings did not desensitize to the TRPs. 4. The relative ...Continue Reading

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Citations

Jul 1, 1997·Thrombosis Research·A RayJ B Gupta
Sep 24, 2002·Pharmacology & Therapeutics·Rommel S LanPeter J Henry
Jan 4, 2012·Nature Reviews. Drug Discovery·Rithwik RamachandranMorley D Hollenberg
Jan 23, 2008·Cancer Cell International·Akiko UedaShunichiro Kubota
Jun 24, 1998·Proceedings of the National Academy of Sciences of the United States of America·N VergnolleM D Hollenberg
Feb 1, 2011·Pharmacology & Therapeutics·Mark N AdamsJohn D Hooper
May 15, 2003·British Journal of Pharmacology·Michele TognettoSelena Harrison
Sep 27, 2005·Vascular Pharmacology·Mariarosaria BucciGiuseppe Cirino
Feb 24, 2001·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·A Kawabata
Nov 14, 1997·Circulation Research·P SchaefferJ M Herbert
Feb 3, 2007·Arteriosclerosis, Thrombosis, and Vascular Biology·Tetsuhiro FujiyoshiHideo Kanaide
Apr 25, 2000·American Journal of Physiology. Heart and Circulatory Physiology·C Fernandez-PatronS T Davidge
Jun 2, 2001·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·C CicalaG Cirino
Sep 4, 2007·American Journal of Physiology. Heart and Circulatory Physiology·Mahmoud SaifeddineMorley D Hollenberg
Aug 3, 2000·American Journal of Physiology. Heart and Circulatory Physiology·Y GuiM D Hollenberg
Feb 22, 2003·American Journal of Physiology. Heart and Circulatory Physiology·John J BosnjakDavid D Gutterman

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