Description
Efonidipine is a mixture of R(-) and S(+) isomers that exerts long acting blocking actions on both T-type and L-type calcium channels. It has no blocking effects on N-, P/Q- and R-type Ca(2+) channels. While the S(+) isomer is an active blocker of both the T-type and L-type calcium channels, the action of which is similar to the racemic mixture, its R(-) isomer selectively blocks the T-type channel only. In the prevention of cardiovascular disease efonidipine inhibits in a dose dependent manner the Ang II- and K+-induced aldosterone secretion. It suppresses Ang-II and K+-induced mRNA expression of 11-beta-hydroxylase and aldosterone synthase and induces the production of DHEA sulfate, which has anti-atherosclerotic actions.
References
Furukawa T.,Miura R,Honda M, et al. Idenfication of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels. Br. J Pharmacol. 2004 Dec; 143(8):1050-7. PIMD:15545287, PMCID:PMC1575949.
Tanaka H, Shigenobu K. Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels. Cardiovascv Drug Rev. 2002 Winter; 20(1):81-92. PMID:12070536.
Imafawa K, Okayama S, Takaoka M, et al Inhibitory effect of efonidipine on aldosterone synthesis and secretion on human adrenocarcinoma (H195R) cells. J Cardiovasc Pharmacol. 2006 Jan; 47(1):133-8. PMID:16424797.
Ikeda K, Saito T, Tojo K. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H195 R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011; 224(4):263-71. PMID:21757861.
