Dilazep (hydrochloride)

Dilazep is an inhibitor of equilibrative nucleoside transporter 1 (ENT1; IC₅₀ = 17.5 nM).¹ It is selective for ENT1 over ENT2 (IC₅₀ = 8,800 nM). Dilazep (0.03 and 0.3 µM) increases adenosine-induced relaxation of, and decreases calcium-induced contractions in isolated guinea pig taenia caeci strips when used at concentrations of 1, 5, and 10 µM.² Dilazep (0.2 mg/kg, i.v.) reduces heart rate and systolic, mean, and diastolic aortic pressure and increases left ventricular blood flow in anesthetized dogs.³ It reduces aortic platelet adhesion and aggregation in a rabbit model of aortic injury-induced thrombosis when administered intravenously at a dose of 0.1 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Playa, H., Lewis, T.A., Ting, A., et al. Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). Bioorg. Med. Chem. Lett. 24(24), 5801-5804 (2014).

2. Tonini, M., Perucca, E., Manzo, L., et al. Dilazep: An inhibitor of adenosine uptake with intrinsic calcium antagonistic properties. J. Pharm. Pharmacol. 35(7), 434-439 (1983).

3. Marzilli, M., Trivella, M.G., Levantesi, D., et al. Effect of dilazep on coronary and systemic circulations. Pharmacology 31(2), 82-87 (1985).

4. Sumiyoshi, A., and Hayashi, T. The inhibitory effect of dilazep on in vivo accumulation of platelets onto the damaged aorta in Rabbit. II. Morphological analysis. Comparative Study 29(1), 37-42 (1983).