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Vasorelaxant effect in rat aortic rings through calcium channel blockage: A preliminary in vitro assessment of a 1,3,4-oxadiazole derivative

Bankar, Girish R and Nandakumar, K and Nayak, Pawan G and Thakur, Anjali and Rao, Mallikarjuna C and Nampurath, Gopalan Kutty (2009) Vasorelaxant effect in rat aortic rings through calcium channel blockage: A preliminary in vitro assessment of a 1,3,4-oxadiazole derivative. Chemico-Biological Interactions , 181 (3). 377-382. ISSN 0009-2797

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Abstract

The study was undertaken on the basis of several reports in the literature that relaxation of vascular smooth muscles is a good treatment strategy in hypertension, angina and other cardiovascular disorders. Oxadiazoles have been reported to have effect on vascular smooth muscles and calcium influx. The goals of our current in vitro study were to investigate the effect of a 1,3,4-oxadiazole derivative on vascular smooth muscles in rat aorta, and to elucidate the associated signaling pathway. NOX-1 induced a relaxation of vascular smooth muscles in both endothelium intact and denuded rat aortic rings precontracted with norepinephrine or phenylephrine or KCl. NOX-1 also significantly antagonized cumulative dose–response effect of norepinephrine, phenylephrine, KCl or calcium with reduction in submaximal contractions. Verapamil, an L-type of calcium channel blocker, effectively attenuated phenylephrine and calcium induced contractions in aortic rings. Incubation with NOX-1 and verapamil did not significantly alter the dose–response curve of phenylephrine or calcium compared to verapamil treatment alone indicating L-type Ca2+ channel blockage leads to loss of NOX-1 activity. Hence it can be concluded NOX-1 exhibited vasorelaxant action by inhibiting calcium influx from extracellular space to intracellular space through L-type of calcium channels.

Item Type: Article
Uncontrolled Keywords: 1,3,4-Oxadiazoles; Vasorelaxation; Aortic rings; Calcium influx;Hypertension.
Subjects: Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 27 Jan 2012 09:47
Last Modified: 24 Dec 2013 06:51
URI: http://eprints.manipal.edu/id/eprint/2711

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