Ethaverine drochloride, a derivative of papaverine, inhibits cardiac L-type calcium channel. Ethaverine drochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine drochloride can be used for research of peripheral vascular disease.
Ethaverine drochloride (10 μM, PC12 cells) reduces catecholamine secretion by blocking the L-type voltage-sensitive Ca2+ channel[2].Ethaverine drochloride (12 h) decreases dopamine content by inhibiting tyrosine droxylase (TH) activity in PC12 cells, with an IC50 of 1.4 μM[3].Ethaverine drochloride inhibits monoamine oxidase (MAO) activity in mouse brain (isolated from mouse whole brain), with an IC50 of 25.5 μM[6].
Ethaverine drochloride (2-10 mg/kg, intravenous infusion, i.v.) causes significant elevation of endocochlear potential in guinea pigs[4].Ethaverine (1-10 mg/kg, i.v.) inhibits atrioventricular conduction and heart rate in the anaesthetized dog[5].
References:
[1]. Wang Y, et al. Ethaverine, a derivative of papaverine, inhibits cardiac L-type calcium channels. Mol Pharmacol. 1991 Nov;40(5):750-5.
[2]. Suh BC, et al. Inhibition by ethaverine of catecholamine secretion through blocking L-type Ca2+ channels in PC12 cells. Biochem Pharmacol. 1994 Mar 29;47(7):1262-6.
[3]. Shin JS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on dopamine content in PC12 cells. Biol Pharm Bull. 2001 Jan;24(1):103-5.
[4]. Prazma J, et al. Effect of ethaverine drochloride on cochlear microcirculation. Arch Otolaryngol. 1981 Apr;107(4):227-9.
[5]. Lacroix P, et al. [Comparative activity of ethaverine and papaverine on chronotropic and dromotropic cardiac functions in the anesthetized dog]. Arch Int Pharmacodyn Ther. 1976 May;221(1):163-76. French.
[6]. Lee SS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on monoamine oxidase activity in mouse brain. Biol Pharm Bull. 2001 Jul;24(7):838-40.