Efonidipine

Efonidipine is an inhibitor of L- and T-type voltage-gated calcium channels (Ca_vs).¹ It inhibits Ca_v1.2a (IC₅₀ = 1.8 nM for the hamster channel), an L-type Ca_v, and Ca_v3.2 (IC₅₀ = 350 nM for the human channel), a T-type Ca_v. It also inhibits L- and T-type calcium channels and fetal bovine serum-induced hypertrophy in isolated mouse cardiomyocytes.² Efonidipine (200 mg/kg) increases survival in a mouse model of acute myocardial infarction induced by ligation of the left coronary artery.³ Efonidipine is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro; IC₅₀ = 38.5 µM).⁴

WARNING This product is not for human or veterinary use.

1. Lee, T.-S., Kaku, T., Takebayashi, S., et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca²⁺ channels with distinct inhibitory mechanisms. Pharmacology 78(1), 11-20 (2006).

2. Horiba, M., Muto, T., Ueda, N., et al. T-type Ca²⁺ channel blockers prevent cardiac cell hypertrophy through an inhibition of calcineurin-NFAT3 activation as well as L-type Ca²⁺ channel blockers. Life Sci. 82(11-12), 554-560 (2008).

3. Kinoshita, H., Kuwahara, K., Takano, M., et al. T-type Ca²⁺ channel blockade prevents sudden death in mice with heart failure. Circulation 120(9), 743-752 (2009).

4. Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al. Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2. ACS Med. Chem. Lett. 11(12), 2526-2533 (2020).