Niguldipine Research Paper

Niguldipine (hydrochloride)

Description:
Ki = 0.16 nM: a potent, selective α1A-adrenoceptor antagonist
IC50s = 0.4 µM: inhibits L-type Ca2+ channels
IC50s = 0.9 µM: suppresses T-type Ca2+ channels

Niguldipine is a less potent Ca2+ channel blocker and potent, selective α1A-adrenoceptor receptor antagonist. Ca2+ channels, expressed in the smooth muscles of the male reproductive tract, play a role in the physiological events involved in the seminal emission phase of ejaculation. It was demonstrated that α1-adrenoceptors, as members of superfamily of G protein-coupled receptors, are not a homogeneous population and have three distinct α1-adrenoceptor subtypes, involving α1A, α1B, and α1D.

In vitro: Niguldipine significantly increased the rate of long-lived protein degradation in human glioblastoma H4 cell, which indicated that niguldipine triggered autophagic degradation without inducing obvious cellular damage. Also, niguldipine blocked intracellular Ca2+ currents [1].
Niguldipine did not affect the electroconvulsive threshold in mice. Compared to the anticonvulsive activity of niguldipine against electroconvulsions, niguldipine remarkably impaired the protective action of both phenobarbital and carbamazepine