Sildenafil citrate Inhibitor CAS No. 171599-83-0

Product Name	Sildenafil citrate
Synonyms	Viagra, UK-92,480
CAS No.	171599-83-0
Molecular Weight	666.7
Formula	C₂₈H₃₈N₆O₁₁S
Chemical Structure
Documents	HNMR COA HPLC MS

Biological activities

Sildenafil citrate is a citrate salt form of sildenafil. Sildenafil is a cGMP-specific phosphodiesterase type 5 (PDE5) inhibitor. The IC50 of sildenafil is 3.9 nM against PDE5.^[1] In soluble extracts of human corpus cavernosum smooth muscle cells, sildenafil effectively susppresses cGMP hydrolysis at substrate concentrations of 1, 5 and 10 µM cGMP. The Ki of sildenafil is 14.7 nM for PDE5. Sildenafil also causes dose-dependent increases in intracellular cGMP.^[2] In another study, it is reported that sildenafil inhibits cGMP hydrolysis concentration-dependently. In guinea pig arteries, sildenafil induces an endothelium-dependent vasodilatation only at concentrations above 10 nM.^[3] Sildenafil relaxes corpus cavernosum smooth muscle by amplifying the effects of the normal, endogenous cGMP dependent relaxation mechanisms.^[4] Sildenafil significantly increases cAMP in both cavernous and cardiac tissue in physiologic and supraphysiologic concentrations.^[5] In the presence or absence of SNP, sildenafil increases cGMP concentrations in rabbit penile tissue with increasing dose.^[6] Sildenafil augments the neuronal mechanism responsible for penile erection.^[7]

Protocols

In vivo: Sildenafil is dissolved in saline and given at doses of 1-100 µg/kg.^[7]

References

[1] Boolell M, et al. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int J Impot Res. 1996, 8(2): 47-52. 閵嗏偓閵嗏偓 [2] Kim NN, et al. Inhibition of cyclic GMP hydrolysis in human corpus cavernosum smooth muscle cells by vardenafil, a novel, selective phosphodiesterase type 5 inhibitor. Life Sci. 2001, 69(19): 2249-2256. 閵嗏偓閵嗏偓 [3] Kruuse C, et al. Phosphodiesterase 5 and effects of sildenafil on cerebral arteries of man and guinea pig. Eur J Pharmacol. 2005, 521(1-3): 105-114. 閵嗏偓閵嗏偓 [4] Chuang AT, et al. Sildenafil, a type-5 CGMP phosphodiesterase inhibitor, specifically amplifies endogenous cGMP-dependent relaxation in rabbit corpus cavernosum smooth muscle in vitro. J Urol. 1998, 160(1): 257-261. 閵嗏偓閵嗏偓 [5] Stief CG, et al. Effects of sildenafil on cAMP and cGMP levels in isolated human cavernous and cardiac tissue. Urology. 2000, 55(1): 146-150. 閵嗏偓閵嗏偓 [6] Jeremy JY, et al. Effects of sildenafil, a type-5 cGMP phosphodiesterase inhibitor, and papaverine on cyclic GMP and cyclic AMP levels in the rabbit corpus cavernosum in vitro. Br J Urol. 1997, 79(6): 958-963. 閵嗏偓閵嗏偓 [7] Carter AJ, et al. Effect of the selective phosphodiesterase type 5 inhibitor sildenafil on erectile dysfunction in the anesthetized dog. J Urol. 1998, 160(1): 242-246. 閵嗏偓閵嗏偓

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