Niguldipine (hydrochloride)

Niguldipine is a dihydropyridine that acts as a potent, selective α_1A-adrenoceptor antagonist (K_i = 0.16 nM).^1,2,3 It less potently blocks L- and T-type Ca²⁺ channels (IC₅₀s = 0.4 and 0.9 µM, respectively).^4,5

WARNING This product is not for human or veterinary use.

1. Li, M.Y., Tsai, K.C., and Xia, L. Pharmacophore identification of α1A-adrenoceptor antagonists. Bioorg. Med. Chem. Lett. 15(3), 657-664 (2005).

2. Bylund, D.B. Subtypes of α1- and α2-adrenergic receptors. The FASEB Journal 6(3), 832-839 (1992).

3. van Rhee, A.M., Jiang, J.L., Melman, N., et al. Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: Selectivity for A₃ receptors. J. Med. Chem. 39(15), 2980-2989 (1996).

4. Klöckner, U., and Isenberg, G. The dihydropyridine niguldipine modulates calcium and potassium currents in vascular smooth muscle cells. Brit. J. Pharmacol. 97(3), 957-967 (1989).

5. Perez-Reyes, E., Van Deusen, A.L., and Vitko, I. Molecular pharmacology of human Ca_v3.2 T-type Ca²⁺ channels: Block by antihypertensives, antiarrhythmics, and their analogs. J. Pharmacol. Exp. Ther. 328(2), 621-627 (2009).