Sildenafil (CAS No. 139755-83-2) yog cov hmoov dawb crystalline hmoov nrog cov mis molecular C22H30N6O4S thiab qhov ceev ntawm 1.39 g / cm3. Nws yog ib qho tshuaj kho mob erectile kawg hauv cov txiv neej, nrhiav pom thaum lub sij hawm tsim cov tshuaj rau cov kab mob plawv. Nws feem ntau paub los ntawm nws lub npe lag luam Viagra. Nws yog ib qho kev xaiv inhibitor ntawm phosphodiesterase (PDE) V, txhim kho cov lus teb physiological ntawm penile erection induced los ntawm TSIS tso tawm nyob rau hauv teb rau kev sib deev stimulation. Nws yog feem ntau siv rau erectile kawg.
Dosage thiab Administration
1. Rau cov neeg mob feem ntau, cov koob tshuaj pom zoo yog 120 mg, noj raws li xav tau kwv yees li 1 teev ua ntej kev sib deev, nrog rau kev sib deev xav tau tom qab kev tswj hwm. Txawm li cas los xij, nws tuaj yeem noj txhua lub sijhawm hauv 0.5-4 teev ua ntej kev sib deev. Raws li kev ua tau zoo thiab kev kam rau siab, koob tshuaj txhua hnub yuav raug hloov mus rau nruab nrab ntawm 150 mg, tab sis yuav tsum tsis txhob noj ntau dua ib hnub.
- Kev noj tshuaj rau lub raum tsis txaus: Kev pom zoo pib koob tshuaj rau cov neeg mob lub raum tsis ua haujlwm hnyav (qhov twg creatinine tshem tawm tsawg dua lossis sib npaug li 30 ml / min, thiab AUC thiab cmax yuav luag ob npaug) yog 25 mg.
- Kev noj tshuaj rau lub siab tsis txaus: Qhov pom zoo pib koob tshuaj rau cov neeg mob uas muaj lub siab tsis zoo (xws li cirrhosis, qhov twg AUC thiab cmax nce 84% thiab 47%, feem) yog 80 mg.
2. Kev siv tshuaj rau cov neeg laus: Qhov pom zoo pib koob tshuaj rau cov neeg mob hnub nyoog 65 xyoo thiab laus dua yog 100 mg.
Product Specifications thiab Properties
- CAS Nr .: 139755-83-2;
- Lub npe tshuaj: Sildenafil;
- Cov mis mos molecular: C22H30N6O4S;
- Purity: 99%;
- Qhov tsos: Dawb hmoov;
- Melting Point: 187-189 degree;
- Txoj Kev Tshawb Nrhiav: Kev Cuam Tshuam Ua Haujlwm Siab Spectrometry;
- Txheem: USP (United States Patent and Trademark Office)
Kev tsim khoom thiab kev siv
Ethyl 3-n-propylpyrazole-5-carboxylate thiab dimethyl sulfate yog sib xyaw thiab ua rau kom tau ethyl 2-methyl-3-n-propylpyrazole5- Qhov no yog tom qab ntawd tshem tawm hauv cov tshuaj sodium hydroxide thiab hydrolyzed kom tau 2-methyl-3-n-propylpyrazole-5-carboxylic acid. Cov khoom siv hydrolysis tau ntxiv rau hauv ib feem rau cov kua qaub sib xyaw thiab nitrated kom tau 1-methyl-4-nitro-3-n-propylpyrazole-5-carboxylic acid. Cov khoom siv nitration yog chlorinated nrog thionyl chloride mus rau acyl chloride, thiab tom qab ntawd aminated nrog concentrated ammonia kom tau 1-methyl-4-nitro-3-n-propylpyrazole-5-carboxamide. Cov carboxamide thiab tin dichloride dihydrate raug tshem tawm hauv ethanol thiab txo qis hauv reflux kom muab 4-amino-1-methyl-3-n-propylpyrazole-5-carboxamide. Cov khoom txo qis, 4-dimethylaminopyridine, thiab triethylamine tau yaj hauv dichloromethane, thiab tom qab ntawd ntxiv cov tshuaj dichloromethane ntawm 2-ethoxybenzoyl chloride, ua raws li acylation muab 4-(2-ethoxybenzoylamino)-1-methyl-3-n-propylpyrazole-5-carboxamide. Cov khoom acylated no tau cyclized hauv aqueous sodium hydroxide thiab hydrogen peroxide kom muab 5-(2-ethoxyphenyl)-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyridin-7-one. Cov khoom siv cyclized tau ntxiv rau hauv feem rau chlorosulfonic acid muab 5-(5-chlorosulfonyl-2-ethoxyphenyl)-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyridin-7-one. Cov khoom chlorosulfonated raug tshem tawm hauv ethanol, thiab 4-methylpiperazine tau ntxiv thiab nplawm kom tau sildenafil.
Mechanism ntawm kev ua
Thaum lub sij hawm kev sib deev stimulation, nitric oxide synthase nyob rau hauv non-adrenergic, non-cholinergic neurons ntawm corpus cavernosum thiab vascular endothelial hlwb catalyzes cov synthesis ntawm nitric oxide los ntawm L-arginine. Nitric oxide activates guanylate cyclase, ua kom cov synthesis ntawm cyclic guanosine monophosphate (cGMP), uas nyob rau hauv lem ua rau so ntawm cov nqaij ntshiv ntawm lub corpus cavernosum thiab cov hlab ntsha me, tso cai rau cov ntshav ntws mus rau hauv lub cavernous sinus thiab ua rau penile erection. Ib txhij, cGMP yog hydrolyzed los ntawm phosphodiesterase.
Yog li, txoj kev xav, ob qho tib si nce kev ua haujlwm ntawm guanylate cyclase thiab inhibiting cov haujlwm ntawm phosphodiesterase tuaj yeem nce qib ntawm cGMP, pab txhawb kev so ntawm cov leeg nqaij ntawm corpus cavernosum thiab cov hlab ntsha me. Viagra (Sildenafil) nce qib cGMP los ntawm inhibiting hydrolytic kev ua ntawm phosphodiesterase yam tsis muaj kev cuam tshuam rau cGMP, yog li ua rau cov nitric oxide synthase / cGMP cascade nyhuv induced los ntawm kev sib deev stimulation, relaxing lub du nqaij ntawm lub corpus cavernosum, thiab ua tiav lub hom phiaj ntawm kev kho erectile kawg.
Vim li cas thiaj xaiv peb
Xaiv peb: Peb muab thawj - tes; lav kev sib tw nqi thiab zoo. Tom qab koj tso ib qho kev txiav txim, peb tuaj yeem npaj cov khoom xa tuaj rau tib hnub, ua kom cov khoom zoo thiab ruaj khov, cia peb koom tes ua cov neeg xa khoom.



