l Inombolo ye-Cas: 171596-29-5 I-Molecular Formula: C₂₂H₁₉N₃O₄

Imikhiqizo

l Inombolo ye-Cas: 171596-29-5 I-Molecular Formula: C₂₂H₁₉N₃O₄

Incazelo emfushane:

Inombolo yeCas: 171596-29-5
Igama Lekhemikhali:
I-Molecular Formula: C₂₂H₁₉N₃O₄
Synonimes: (6R,12aR)-6-(1,3-Benzodioxol-5-yl) -2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6] i-pyrido[3,4-b]indole-1,4-dione;GF 196960;I-IC 351;I-ICOS 351;I-Tildenafil;UK 336017;


Imininingwane Yomkhiqizo

Omaka bomkhiqizo

imininingwane yemikhiqizo

I-Melting Point > 193°C
Ukuminyana I-DMF: 25 mg/ml
I-DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml
I-DMSO: 20 mg/ml
izinga lokushisa lokugcina -20°C
ukuncibilika I-DMF: 25 mg/ml
I-DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml
I-DMSO: 20 mg/ml
umsebenzi optical [α]/D +68 kuya +78°, c = 1 ku-chloroform-d
Ukubukeka Okuqinile Okumhlophe kuya Kokumhlophe
Ubumsulwa ≥98%

Imikhiqizo Pharmacology

(igama lemakethe noma ) uhlobo lwe-PDE5 inhibitor esetshenziselwa ukwelapha ukungasebenzi kahle kwe-erectile, i-benign prostatic hypertrophy kanye ne-pulmonary arterial hypertension.Umphumela uwukuphumuza imisipha yemithambo yegazi nokwandisa ukugeleza kwegazi ku-corpus cavernosum.Indlela yokusebenza ye-inhibiting umsebenzi we-cGMP ethize phosphodiesterase hlobo 5 (PDE5).I-PDE5 yehlisa isithunzi i-cGMP ku-corpus cavernosum etholakala eduze komthondo.Ngakho-ke, i-tadalafi iholela ekwandeni kokuhlushwa kwe-cGMP okuphinde kubangele ukuphumula kwemisipha ebushelelezi kanye nokukhuphuka kwegazi ku-corpus cavernosum.Ezinye izifundo zomtholampilo ziphinde zasikisela ukuthi zingathuthukisa ukusebenza kwe-endothelia emadodeni anengozi eyandayo yenhliziyo nemithambo yegazi futhi ehlise izimpawu zepheshana lomchamo okwesibili ku-benign prostatic hyperplasia.

imikhiqizo Sebenzisa

i-analgesic, i-uptake blocker, i-mu-opiod receptor agonist.I-phosphodiesterase 5 inhibitor.isetshenziselwa ukwelapha ukungasebenzi kahle kwe-erectile.

Ukusetshenziswa kanye Nesilinganiso

ihluke ngesakhiwo kusuka kokubili i-sildenafil ne-vardenafil.Imuncwa ngokushesha futhi inyuke kakhulu ekugxilweni kwayo (378 μg/L ngemva komthamo we-20-mg) ngemva kwamahora ama-2, ibonise isigamu sempilo ende yamahora angu-17.5.Iphinde isetshenziswe isibindi (CYP3A4).Ngokuphawulekayo, i-pharmacokinetics yayo ayithonywa ngokomtholampilo utshwala noma ukudla noma izinto ezifana nesifo sikashukela noma ukungasebenzi kahle kwesibindi noma izinso.

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