Vardenafil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

伐地那非（艾力达）是一种治疗勃起功能障碍的口服疗法。

Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM.Vardenafil increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow.

Vardenafil (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury.Vardenafil (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.Vardenafil (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. Animal Model:Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury Dosage:0.03 mg/kg.Administration:Intravenous injection Result:Restored normal erectile responses with a combind administration of BAY 60-4552 (0.03, 0.3 mg/kg).Animal Model:Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g) Dosage:0.17 mg/kg Administration:Intravenous injection; once daily for 7 days; as a pretreatment Result:Reduced the levels of serum transaminases and alleviated Con A-induced hepatitis.Animal Model:Male 7-week-old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)Dosage:10 mg/kg Administration:Oral gavage; once daily, for 25 weeks Result:Improved myofilament function in diabetic rat hearts.

Vardenafil | Levitra | Staxyn | Vivanza | BAY 38-9456

Angiogenesis

PDE

PDE1| PED5

Endocrinology

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224785-90-4

579.11

C23H32N6O4S·HCl·3H2O

>98% (HPLC)

Ethanol: 20 mg/mL (34.53 mM); Water: 116 mg/mL (200.3 mM); DMSO: 116 mg/mL (200.3 mM)

O=C(NC(C1=CC(S(=O)(N2CCN(CC)CC2)=O)=CC=C1OCC)=N3)[N]4(C)C3=CN(CCC)C4

2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propyl-3,5,6,7-tetrahydro-4H-5l4-imidazo[1,5-a][1,3,5]triazin-4-one

(-20℃)

With Ice Pack

≥ 2 years