(±)-Verapamil hydrochloride 

α₁-adrenoceptor antagonist; L-type calcium channel blocker. Blocks L-type Ca²⁺ channels in smooth and cardiac muscle, induces apoptosis of human primary and metastatic colon adenocarcinoma cells in vitro. Drug resistance reversal agent acting on Pgp, e.g. decrease renal tubule elimination of digoxin. Increases basal ATPase activity of Pgp. Substrate of Cyp3A4 and CYP2C6.

≥99.0% (titration)

powder

white

142 °C (dec.)(lit.)

H₂O: 50 mg/mL

ethanol: soluble

human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)

Atlas, D., Adler, M., α-Adrenergic antagonists as possible calcium channel inhibitors. Proc. Natl. Acad. Sci. USA 78, 1237, (1981)

Scharff, Effect of trifluoperazine compund 48/80TMB-8 and verapamil on the rate of calmodulin binding to erythrocyte Ca²⁺-ATPase. Biochim. Biophys. Acta 772, 29, (1984)

Goodman and Gilman Goodman and Gilman’s The Pharmacological Basis of Therapeutics 8th ed., New York, NY, USA , 774, (1990)

Fleckenstein, A., Specific pharmacology of calcium in myocardium, cardiac pacemakers, and vascular smooth muscle. Annu. Rev. Pharmacol. 17, 149, (1977)

He, L., et al., Acta Pharmacol Sin. . Transition Metals for Organic Synthesis 23, 423-429, (2002)

Verschraagen, M., et al. Pharmacol. Res. 40, 301-306, (1999)

Kantola, T., et al. Clin. Pharmacol. Ther. 64, 177-182, (1998)

Stringer, K.A., et al. Eur. J. Clin. Pharmacol. 43, 35-38, (1992)

Achira, M., et al., AAPS PharmSci. Transition Metals for Organic Synthesis 1, E18, (1999)

Janis, R., et al. Adv. Drug Res. 16, 309, (1987)

Merck 13,10012

FT-IR 2 (2), 3113:D / RegBook 1 (2), 2107:K / Structure Index 1, 333:E:4

UN 2811 6.1/PG 3

3

YV8320000