Niguldipine HCl has been reported to be a highly selective α 1-adrenoceptor antagonist and dihydropyridine calcium channel blocker. More specifically, Niguldipine HCl has been shown to irreversibly inhibit T-type calcium channel currents in certain types of central and peripheral neurons and in smooth muscle cells. This compound has also been noted to inhibit noradrenaline-stimulated inositol phosphate accumulation. Additional reports demonstrate that Niguldipine HCl can potently and specifically inhibit bTREK-1 (IC50 = 5.07μM). Niguldipine HCl is an inhibitor of Mdr-1.
1. Robinson, J.P., et al. 1990. Br. J. Pharmacol. 100: 3-4. PMID: 2164859
2. Höllt, V., et al. 1992. Biochem. Pharmacol. 43: 2601-2608. PMID: 1352973
3. Stengel, W., et al. 1998. Eur. J. Pharmacol. 342: 339-345. PMID: 9548406
4. Liu, H., et al. 2007. J. Pharmacol. Exp. Ther. 323: 39-48. PMID: 17622574