Supply Sildenafil Powder Original Manufacturer Supply CAS 139755-83-2 Sildenafil Powder
2. Sildenafil effect:
Sildenafil is Viagra.
It is a V-phosphodiesterase inhibitor for the treatment of erectile dysfunction.
3.【Pharmacology and Toxicology】
Sildenafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) specific for cyclic guanosine monophosphate (cGMP). Can be used to treat erectile dysfunction (ED). 1. Mechanism of Action The physiological mechanism of penile erection involves the release of nitric oxide (NO) from the corpus cavernosum during sexual stimulation. NO activation of guanylate cyclase leads to an increase in the level of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle in the cavernosal and causes blood to fill. 2. Pharmacodynamics (1) The effect of sildenafil on penile erection response. Sildenafil is a highly selective inhibitor of phosphodiesterase 5 (PDE5), which is highly expressed in the corpus cavernosum, but is underexpressed in other tissues (including platelets, blood vessels, and visceral smooth muscle, skeletal muscle). Sildenafil selectively inhibits PDE5, enhances the nitric oxide (NO)-cGMP pathway, increases the level of cGMP and leads to the relaxation of the smooth muscle of the corpus cavernosum, so that patients with erectile dysfunction have a natural erectile response to sexual stimulation. Erectile response generally increases with increasing dose and plasma concentration of sildenafil. Experiments show that the drug effect can last up to 4 hours, but the response is weaker than that at 2 hours. (2) The response of sildenafil to the myocardium. PDE5 does not exist in normal or diseased cardiac conduction tissue, cardiomyocytes, endothelial cells, and lymphoid tissue, so sildenafil (PDE5 inhibitor) has no positive inotropic effect and cannot directly affect myocardial contractile function. (3) The effect of sildenafil on cardiac parameters. Normal male volunteers received a single oral dose of sildenafil 100 mg, and no clinically significant ECG changes occurred. Under the monitoring of Swan-Ganz catheter, 8 patients with stable ischemic heart disease received a total of 40 mg of sildenafil intravenously in 4 divided doses. The results showed that the systolic and diastolic blood pressure of the patients at rest were higher than those at baseline. down 7% and 10%. Resting right atrium, pulmonary artery pressure, pulmonary artery wedge pressure, and cardiac output decreased on average by 28%, 28%, 20%, and 7%, respectively. Although this intravenous dose was 2 to 5 times higher than the mean peak plasma concentration of a single oral dose of sildenafil 100 mg in healthy male volunteers, the above-mentioned hemodynamic response persisted during exercise.
3-n-propylpyrazole-5-carboxylate ethyl ester and dimethyl sulfate are mixed to obtain 2-methyl-3-n-propylpyrazole-5-carboxylate ethyl ester. It is suspended in sodium hydroxide solution and hydrolyzed to obtain 2-methyl-3-n-propylpyrazole-5-carboxylic acid. The hydrolyzed product was added to the mixed acid in batches and nitration to obtain 1-methyl-4-nitro-3-n-propylpyrazole-5-carboxylic acid. The nitrated product is chlorinated into acid chloride with thionyl chloride, and then ammoniated with concentrated ammonia to obtain 1-methyl-4-nitro-3-n-propylpyrazole-5-carboxamide. The carboxamide and tin dichloride dihydrate are suspended in ethanol and reduced by reflux to obtain 4-amino-1-methyl-3-n-propylpyrazole-5-carboxamide. The reduced product, 4-dimethylaminopyridine and triethylamine are dissolved in dichloromethane, and then the dichloromethane solution of 2-ethoxybenzoyl chloride is added to obtain 4-(2-ethoxybenzyl chloride) after acylation. amido)-1-methyl-3-n-propylpyrazole-5-carboxamide. The acylated product was cyclized under the action of aqueous sodium hydroxide and hydrogen peroxide to obtain 5-(2-ethoxyphenyl)-1-methyl-3-n-propyl-1,6-dihydro-7H-pyridine Azolo[4,3-d]pyridin-7-one. The cyclization product was added to chlorosulfonic acid in batches to give 5-(5-chlorosulfo-2-ethoxyphenyl)-1-methyl-3-n-propyl 1,6-dihydro-7H- Pyrazolo[4,3-d]pyridin-7-one. The chlorosulfonated product was suspended in ethanol, 4-methylpiperazine was added, and sildenafil was obtained by stirring.