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Vardenafil HCl Trihydrate

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Chemical Structure| 330808-88-3 同义名 : 盐酸瓦地那非三水合物 ;Vardenafil (hydrochloride hydrate);BAY38-9456;Vivanza;Staxyn;Levitra;Vardenafil HCl;Vardenafil HCl Trihydrate
CAS号 : 330808-88-3
货号 : A194638
分子式 : C23H39ClN6O7S
纯度 : 98%
分子量 : 579.11
MDL号 : MFCD08458876
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • PDE5

    PDE5, IC50:0.7 nM
描述 Phosphodiesterase-5 (PDE5) is 1 of 11 mammalian PDE families known to date. PDE5 is a cGMP-specific PDE and is abundant in most smooth muscle tissues as well as in platelets, gastrointestinal epithelial cells, and Purkinje cells of the cerebellum[3]. Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM. In contrast, the IC50 of vardenafil for PDE1 is 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM[4]. Vardenafil significantly enhanced the sodium nitroprusside (SNP)-induced relaxation of human trabecular smooth muscle at 3 nM. It also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle[4]. In vivo studies in rabbits showed that orally administered vardenafil dose-dependently potentiated erectile responses to intravenously administered SNP. The minimal effective dose that significantly potentiated erection was 0.1 mg/kg. The selectivity for PDE5, the potentiation of NO-induced relaxation and cGMP accumulation in human trabecular smooth muscle and the ability to enhance NO-induced erection in vivo indicated that vardenafil had the appropriate properties to be a potential compound for the treatment of erectile dysfunction[4]. Rats treated with vardenafil showed an improved object discrimination performance. Compared with sildenafil, vardenafil appeared to be even more potent in this respect since it already produced a high discrimination performance at a dose of 0.3 mg/kg[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01063855 Erectile Dysfunction ... 展开 >> Sexual Dysfunction 收起 << Phase 3 Completed - -
NCT01063855 - Completed - -
NCT00767598 Pharmacokinetics of Three PDE5... 展开 >>Is Healthy Subjects Genetic Polymorphic CYP3A5 收起 << Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.63mL

1.73mL

0.86mL

17.27mL

3.45mL

1.73mL
参考文献

[1]Blount MA, Beasley A, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52.

[2]Prickaerts J, van Staveren WC, et al. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat. Neuroscience. 2002;113(2):351-61.

[3]Blount MA, Beasley A, Zoraghi R, Sekhar KR, Bessay EP, Francis SH, Corbin JD. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52. doi: 10.1124/mol.66.1.144. PMID: 15213306.

[4]Saenz de Tejada I, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, Körschen HG, Niewöhner U, Haning H, Pages E, Bischoff E. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90. doi: 10.1038/sj.ijir.3900726. PMID: 11890515.

[5]Prickaerts J, van Staveren WC, Sik A, Markerink-van Ittersum M, Niewöhner U, van der Staay FJ, Blokland A, de Vente J. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat. Neuroscience. 2002;113(2):351-61. doi: 10.1016/s0306-4522(02)00199-9. PMID: 12127092.