Vardenafil hydrochloride trihydrate  (Synonyms: 伐地那非盐酸盐水合物)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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-𝜅B 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

579.11

C₂₃H₃₉ClN₆O₇S

330808-88-3

固体

White to off-white

伐地那非盐酸盐水合物

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Saenz de Tejada I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001;13(5):282-290.  [Content Brief]

  [2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.  [Content Brief]

  [3]. Gresser U, et al. Erectile dysfunction: comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil--review of the literature. Eur J Med Res. 2002 Oct 29. 7(10):435-46.  [Content Brief]

  [4]. Oudot A, et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov. 60(5):1020-6.  [Content Brief]

  [5]. Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31(3).  [Content Brief]

  [6]. Bódi B, et al. Long-Term PDE-5A Inhibition Improves Myofilament Function in Left and Right Ventricular Cardiomyocytes through Partially Different Mechanisms in Diabetic Rat Hearts. Antioxidants (Basel). 2021 Nov 6. 10(11):1776.  [Content Brief]