Cardamonin is a bifunctional vasodilator that inhibits Ca(v)1.2 current and stimulates K(Ca)1.1 current in rat tail artery myocytes

The Journal of Pharmacology and Experimental Therapeutics
Fabio FusiSimona Saponara

Abstract

An in-depth analysis of the effects of cardamonin, 2',4'-dihydroxy-6'-methoxychalcone, on rat tail artery preparations was performed by means of whole-cell patch-clamp recordings of Ca(v)1.2 Ca(2+) [I(Ca(L))] or Ba(2+) [I(Ba(L))] current as well as K(Ca)1.1 currents in single myocytes and by measuring contractile responses in endothelium-denuded isolated rings. At a holding potential (V(h)) of -80 mV, cardamonin decreased both I(Ba(L)) and I(Ca(L)) in a concentration-dependent manner with similar pIC(50) values. The maximum of the I(Ba(L))-voltage relationship was shifted by 10 mV in the hyperpolarizing direction, but threshold remained unaffected. Cardamonin modified both the activation and the inactivation kinetics of I(Ba(L)) and shifted the voltage dependence of both inactivation and activation curves to more negative potentials by 19 and 7 mV, respectively, thus markedly decreasing the Ba(2+) window current. Block of I(Ba(L)) was frequency-dependent, and rate of recovery from inactivation was slowed. Cardamonin increased K(Ca)1.1 currents in a concentration-dependent manner; this stimulation was iberiotoxin- and BAPTA [1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid]-sensitive. On the contrary, iberiotoxin did not...Continue Reading

References

Oct 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·B P Bean
Aug 1, 1981·Pflügers Archiv : European journal of physiology·O P HamillF J Sigworth
Apr 1, 1995·The American Journal of Physiology·M T Nelson, J M Quayle
Feb 14, 1998·Journal of Natural Products·H DougT Namba
Jan 5, 2001·British Journal of Pharmacology·P Petkova-KirovaR Schubert
May 5, 2001·Journal of Cardiovascular Pharmacology·Z T WangY Huang
Apr 6, 2002·British Journal of Pharmacology·Simona SaponaraFabio Fusi
Aug 2, 2002·Microcirculation : the Official Journal of the Microcirculatory Society, Inc·Robert H Cox, Nancy J Rusch
Nov 5, 2002·Trends in Pharmacological Sciences·Steffen Hering
Nov 18, 2003·Naunyn-Schmiedeberg's Archives of Pharmacology·Fabio FusiGiampietro Sgaragli
Jul 31, 2004·Journal of the American Society of Nephrology : JASN·Dierk H Endemann, Ernesto L Schiffrin
Oct 7, 2004·European Journal of Pharmacology·Jean-Claude StocletValérie B Schini-Kerth
Sep 27, 2005·The Journal of Pharmacology and Experimental Therapeutics·Jeong-Hyung LeeJung Joon Lee
Jan 24, 2006·Vascular Pharmacology·Swapnil SonkusareNancy J Rusch

❮ Previous
Next ❯

Citations

Jan 18, 2014·Journal of Medicinal Food·Luís Moreira GonçalvesJosé António Rodrigues
May 21, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Francisco J Luna-VázquezMiguel Angel Zavala-Sánchez
Oct 26, 2011·Phytochemical Analysis : PCA·Ana M CarvalhoAquiles A Barros
Dec 26, 2016·European Journal of Pharmacology·Fabio FusiSimona Saponara
Jul 17, 2010·Cardiovascular Therapeutics·Eberhard P ScholzChristoph A Karle
Mar 18, 2021·European Journal of Pharmacology·Simona SaponaraMassimo Valoti
Apr 4, 2021·International Journal of Molecular Sciences·Anna Bartáková, Marie Nováková
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rosa Edith Grijalva-GuizaLuis Ricardo Hernández

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.