Background:

PCA50941 is a 1,4-dihydropyridine derivative, used for treatment for cardiovascular disease.

PCA50941 (1 μM) shifts the I-V relationship of whole-cell Ca2+ currents by about 5-10 mV towards more hyperpolarizing potentials. PCA50941 increases further the K(+)-evoked peak to 655 nM. In the presence of 5 mM Ca2+, PCA50941 increases the [Ca2+] peaks to 427 nM. PCA50941 potentiates the release of catecholamines from perfused bovine adrenal glands evoked by 30 s pulses of 17.7 mM K+ in a manner dependent on the [Ca2+]o[1].

PCA50941 (10-120 μM) by intracoronary injection, causes smaller reductions of coronary blood flow (CBF) in goats. PCA50941 (10-300 μM/min) does not modify CBF nor the other hemodynamic variables recorded by i.v. infusions in 4 goats. Intravenous infusion of PCA50941 (100 microg/min) reverses the hemodynamic variables from the shock state to control values within 20 min in 5 of 6 animals[2].

[1]. Montiel C, et al. Interactions between Ca2+, PCA50941 and Bay K 8644 in bovine chromaffin cells. Eur J Pharmacol. 1994 Aug 16;268(3):293-303. [2]. Fernández N, et al. PCA50941, a new 1,4-dihydropyridine, reverses endothelin-induced cardiogenic shock in the anesthetized goat. Life Sci. 1998;62(21):1933-42.