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

≥98%

Store at -20℃

B 844-39;NSC 617553;

1.Li, M.Y.,Tsai, K.C. and Xia, L. Pharmacophore identification of α_1A-adrenoceptor antagonists. Bioorganic & Medicinal Chemistry Letters 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. Journal of Medicinal Chemistry 39(15), 2980-2989 (1996).

4.Klöckner, U. and Isenberg, G. The dihydropyridine niguldipine modulates calcium and potassium currents in vascular smooth muscle cells. British Journal of Pharmacology 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. Journal of Pharmacology and Experimental Therapeutics 328(2), 621-627 (2009).