330808-88-3 Usage
Uses
Used in Pharmaceutical Industry:
Vardenafil hydrochloride trihydrate (subject to patent free) is used as a therapeutic agent for the treatment of erectile dysfunction. It enhances erectile function by increasing intracavernous pressure and mean arterial pressure, with the effect persisting for at least two weeks after the end of treatment.
Additionally, vardenafil hydrochloride trihydrate (subject to patent free) is used as a therapeutic agent for pulmonary arterial hypertension and lower urinary tract dysfunction. Its PDE5 inhibitory properties make it a promising candidate for these conditions, potentially improving the quality of life for patients suffering from these medical issues.
Biological Activity
Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
in vitro
Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.
in vivo
Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio.Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening.
references
[1] saenz de tejada i1, angulo j, cuevas p, fernández a, moncada i, allona a, lledó e, k?rschen hg, niew?hner 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.
Check Digit Verification of cas no
The CAS Registry Mumber 330808-88-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,0,8,0 and 8 respectively; the second part has 2 digits, 8 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 330808-88:
(8*3)+(7*3)+(6*0)+(5*8)+(4*0)+(3*8)+(2*8)+(1*8)=133
133 % 10 = 3
So 330808-88-3 is a valid CAS Registry Number.
