Vardenafil-d₅ hydrochloride  (Synonyms: 盐酸伐地那非-d₅)

Vardenafil-d₅ hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride 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 competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels^[2]. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Vardenafil hydrochloride 特异性抑制 PDE5 对 cGMP 的水解，IC₅₀ 为 0.7 nM^[2]。
Vardenafil hydrochloride 增加阴茎海绵体组织中的细胞内 cGMP 水平，从而导致身体鼻窦扩张和血流量增加^[4]。

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

Vardenafil hydrochloride (IV；0.03 mg/kg) 对海绵体神经损伤大鼠具有促进作用^[5]。
Vardenafil hydrochloride (IV；0.17 mg/kg，每天一次；7 天) 保护肝脏对抗 Con A 诱导的肝炎，并降低肝组织中 NF-^[6]。
Vardenafil hydrochloride (口服；10 mg/kg，每日一次；25 周) 防止组织 cGMP 水平的降低和 ZDF 心脏中 3-NT 生成的增加^[7]。

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

530.09

C₂₃H₂₈D₅ClN₆O₄S

盐酸伐地那非-d₅；瓦地拉非盐酸盐-d₅；伐地那非盐酸盐-d₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. 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]

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

  [4]. 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]

  [5]. 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]

  [6]. 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]

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