Milrinone-d₃

Milrinone-d₃ is intended for use as an internal standard for the quantification of milrinone (Item No. 13357) by GC- or LC-MS. Milrinone is an inhibitor of type 3 phosphodiesterases (PDEs), inhibiting recombinant PDE3A and PDE3B with IC₅₀ values of 0.45 and 1 μM, respectively.¹ It is selective for PDE3 over PDE1, PDE2, PDE4, PDE5, and PDE7 (IC₅₀s = 263, >300, 17.5, 49.1, and 58.3 μM, respectively).¹ Milrinone (0.1-1 mg/kg) has positive inotropic effects, increasing cardiac contractile force in anesthetized dogs with a concomitant increase in heart rate but not blood pressure.² It also increases contractile force in models of propranolol- and verapamil-induced heart failure in anesthetized dogs when administered at an initial dose of 30 µg/kg followed by a continuous 3 µg/kg per minute infusion. Milrinone has vasodilatory effects as well, decreasing mean aortic pressure and increasing venous compliance in anesthetized dogs when administered at an initial dose of 10 µg/kg followed by a continuous 1.7-2.4 µg/kg per minute infusion.³ Formulations containing milrinone have been used in the treatment of heart failure.

WARNING This product is not for human or veterinary use.

1. Sudo, T., Tachibana, K., Toga, K., et al. Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phophodiesterase isozyme activity. Biochem. Pharmacol. 59(4), 347-356 (2000).

2. Alousi, A.A., Canter, J.M., Montenaro, M.J., et al. Cardiotonic activity of milrinone, a new and potent cardiac bipyridine, on the normal and failing heart of experimental animals. J. Cardiovasc. Pharmacol. 5(5), 792-803 (1983).

3. Lee, R.W., Gay, R.G., Lancaster, L.D., et al. Dog model to study the effects of pharmacologic agents on the peripheral circulation: Effects of milrinone. J. Pharmacol. Exp. Ther. 240(3), 1014-1019 (1987).