Vardenafil (hydrochloride trihydrate)

Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4^[1]. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels^[2]. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6]. IC50 & Target:IC50: 0.7 nM (PDE5); 180 nM (PDE1); 11 nM (PDE6); >1000 nM (PDE3, PDE4)^[1] In Vitro: Vardenafil hydrochloride trihydrate specifically inhibits the hydrolysis of cGMP by PDE5 with an IC₅₀ of 0.7 nM^[1].
Vardenafil hydrochloride trihydrate increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow^[3].
In Vivo: Vardenafil hydrochloride trihydrate (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury^[4].
Vardenafil hydrochloride trihydrate (I.V.; 0.17 mg/kg once daily; 7 days) protects liver against Con A-induced hepatitis, and decreases the expression of NF-??B and iNOS in hepatic tissue^[5].
Vardenafil hydrochloride trihydrate (P.O.; 10 mg/kg once daily; 25 weeks) prevents the reduction of tissue cGMP levels and the increase in 3-NT generation in ZDF hearts^[6].