Silodosin-d4 (Synonyms: KMD-3213-d4)

Silodosin-d₄ is intended for use as an internal standard for the quantification of silodosin by GC- or LC-MS. Silodosin is an α_1A-adrenergic receptor (α_1A-AR) antagonist (K_i = 0.036 nM).¹ It is 583- and 56-fold selective for α_1A- over α_1B- and α_1D-ARs, respectively. Silodosin inhibits phenylephrine-induced contraction of isolated rabbit prostate (pA₂ = 10.05) more potently than rabbit or rat aorta (pA₂s = 9.36 and 8.13, respectively).² It inhibits norepinephrine-induced contraction of isolated human prostate tissue when used at concentrations ranging from 0.3 to 10 nM.¹ Silodosin (0.01-1,000 µg/kg) inhibits phenylephrine-induced increases in intraurethral pressure in rats.³ Formulations containing silodosin have been used in the treatment of benign prostatic hyperplasia.

1.Moriyama, N., Akiyama, K., Murata, S., et al.KMD-3213, a novel α1A-adrenoceptor antagonist, potently inhibits the functional α1-adrenoceptor in human prostateEur. J. Pharmacol.331(1)39-42(1997) 2.Yamagishi, R., Akiyama, K., Nakamura, S., et al.Effect of JMD-3213, an α1a-adrenoceptor-selective antagonist, on the contractions of rabbit prostate and rabbit and rat aortaEur. J. Pharm.315(1)73-79(1996) 3.Akiyama, K., Hora, M., Tatemichi, S., et al.KMD-3213, a uroselective and long-acting α1a-adrenoceptor antagonist, tested in a novel rat modelJ. Pharmacol. Exp. Ther.291(1)81-91(1999)