Efonidipine

Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC₅₀ values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis^{[1][2][3][4][5]}. In Vitro:Efonidipine (10 μM, 24 h) induces an increase in StAR mRNA that is independent of extracellular Ca²⁺ in NCI-H295R human adrenocortical cells^[2].
Efonidipine (1 μM, 24 h) significantly increases the production of DHEA-S in NCI-H295R human adrenocortical cells^[2].
In Vivo:Efonidipine (0.1% in diet, p.o., 4 weeks) inhibits T type calcium channels and improves cardiac function during the progression of heart failure in UM-X7.1 hamsters and gold hamsters^[1].