[2H7]-Alfuzosin

Biological Activity

Alfuzosin-d7 is intended for use as an internal standard for the quantification of alfuzosin by GC- or LC-MS. Alfuzosin is an antagonist of α1-adrenergic receptors (α1-ARs; Kis = 10, 10, and 3.16 nM for α1A-, α1B-, and α1D-ARs, respectively).1 It increases the amount of phenylephrine needed to increase urethral and arterial blood pressure in pithed rats when administered at a dose of 10 mg/kg.2 Formulations containing alfuzosin have been used in the treatment of benign prostatic hyperplasia.

References

1.Kenny, B.A., Miller, A.M., Williamson, I.J.R., et al.Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: Binding, functional and in vivo studiesBr. J. Pharmacol.118(4)871-878(1996) 2.Martin, D.J., Lluel, P., Pouyet, T., et al.Relationship between the effects of alfuzosin on rat urethral and blood pressures and its tissue concentrationsLife Sci.63(3)169-176(1998)