Nicardipine (hydrochloride)

Nicardipine is a dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity.¹ It is reported to inhibit adenosine A₁, A_2A, and A₃ receptors with K_i values of 19.6, 63.8, and 3.25 µM, respectively, and can inhibit cytochrome P450 3A4 catalytic activity with an IC₅₀ value of 0.148 µM.^2,3 Additionally, nicardipine has been shown to activate transient receptor potential A1 channels, producing an increase in Ca²⁺ (EC₅₀ = 0.5 µM).⁴

WARNING This product is not for human or veterinary use.

1. Triggle, D.J., and Rampe, D. 1,4-Dihydropyridine activators and antagonists: Structural and functional distinctions. Trends Pharmacol. Sci. 10(12), 507-511 (1989).

2. 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).

3. Stresser, D.M., Blanchard, A.P., Turner, S.D., et al. Substrate-dependent modulation of CYP3A4 catalytic activity: Analysis of 27 test compounds with four fluorometric substrates. Drug Metab. Dispos. 28(12), 1440-1448 (2000).

4. Baraldi, P.G., Preti, D., Materazzi, S., et al. Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents. J. Med. Chem. 53(14), 5085-5107 (2010).