Description
Niguldipine HCl (119934-51-9) is an L-type calcium channel blocker (IC50 = 75 nM), which can also inhibit T-type calcium channels at higher concentrations (IC50 = 244 nM). Novel inhibitor of drug transport by p-glycoprotein.
Uses
Niguldipine Hydrochloride is a selective α 1-adrenoceptor antagonist. Also, it is a new calcium antagonist.
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].
in vivo
female albino swiss mice were administered intraperitoneally in a volume of 10 ml/kg niguldipine for 30 min. 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 [2].
IC 50
s = 0.4 μm: inhibits l-type ca2+ channels
References
1) Stengel et al. (1998), Different potencies of dihydropyridine derivatives in blocking T-type but not L-type Ca2+ channels in neuroblastoma-glioma hybrid cells; Eur. J. Pharmacol., 342 339
2) Hollt et al. (1992), Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein; Biochem. Pharmacol., 43 2601
