Vasorelaxant effect in rat aortic rings through calcium channel blockage

A preliminary in vitro assessment of a 1,3,4-oxadiazole derivative

Girish R. Bankar, K. Nandakumar, Pawan G. Nayak, Anjali Thakur, Mallikarjuna Rao Chamallamudi, Gopalan Kutty Nampurath

Research output: Contribution to journalArticle

28 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)377-382
Number of pages6
JournalChemico-Biological Interactions
Volume181
Issue number3
DOIs
Publication statusPublished - 30-10-2009

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Calcium Channels
Vasodilator Agents
Rats
Phenylephrine
Vascular Smooth Muscle
Muscle
Calcium
Derivatives
Verapamil
L-Type Calcium Channels
Norepinephrine
Intracellular Space
Oxadiazoles
Calcium Channel Blockers
Extracellular Space
Endothelium
Aorta
1,3,4-oxadiazole
In Vitro Techniques
Hypertension

All Science Journal Classification (ASJC) codes

  • Toxicology

Cite this

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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.; Nandakumar, K.; Nayak, Pawan G.; Thakur, Anjali; Chamallamudi, Mallikarjuna Rao; Nampurath, Gopalan Kutty.

In: Chemico-Biological Interactions, Vol. 181, No. 3, 30.10.2009, p. 377-382.

Research output: Contribution to journalArticle

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