l Inombolo yeCas: 171596-29-5 Ifomula yeMolekyuli: C₂₂H₁₉N₃O₄

Iimveliso

l Inombolo yeCas: 171596-29-5 Ifomula yeMolekyuli: C₂₂H₁₉N₃O₄

Inkcazelo emfutshane:

Inombolo yeCas: 171596-29-5
Igama leMchiza:
Ifomula yemolekyuli: C₂₂H₁₉N₃O₄
Izithethantonye: (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6] ipyrido[3,4-b]indole-1,4-dione;GF 196960;I-IC 351;I-ICOS 351;iTildenafil;UK 336017;


Iinkcukacha zeMveliso

Iithegi zeMveliso

ukucaciswa kweemveliso

Indawo yokunyibilika >193°C
Ukuxinana I-DMF: 25 mg / ml
I-DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml
I-DMSO: 20 mg / ml
ixesha lokugcina -20°C
ukunyibilika I-DMF: 25 mg / ml
I-DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml
I-DMSO: 20 mg / ml
umsebenzi wamehlo [α]/D +68 ukuya +78°, c = 1 kwi-chloroform-d
Imbonakalo Mhlophe ukuya kuMhlophe Okuqinileyo
Ubunyulu ≥98%

Iimveliso Pharmacology

(igama lemarike okanye ) luhlobo lwe-PDE5 inhibitor esetyenziselwa unyango lwe-erectile dysfunction, i-benign prostatic hypertrophy kunye ne-pulmonary arterial hypertension.Umphumo wokuphumza imithambo yegazi kunye nokwandisa ukuhamba kwegazi kwi-corpus cavernosum.Indlela yokusebenza ngokuthintela umsebenzi we-cGMP uhlobo oluthile lwe-phosphodiesterase 5 (PDE5).I-PDE5 ithoba i-cGMP kwi-corpus cavernosum ejikeleze ipipi.Ke ngoko, i-tadalafi ikhokelela ekunyukeni koxinzelelo lwe-cGMP ebangela ngakumbi ukuphumla kwemisipha kunye nokwanda kokuhamba kwegazi kwi-corpus cavernosum.Olunye uphononongo lweklinikhi lukwabonisa ukuba kunokuphucula ukusebenza kwe-endothelia kumadoda anomngcipheko owonyukileyo wentliziyo kunye nokwehlisa iimpawu zendlela yomchamo kwi-benign prostatic hyperplasia.

iimveliso Sebenzisa

i-analgesic, i-blocker yokuthatha, i-agonist ye-mu-opiod receptor.I-phosphodiesterase 5 inhibitor.isetyenziselwa unyango lwe-erectile dysfunction.

Ukusetyenziswa kunye nomthamo

ihluke kwisakhiwo esivela kwi-sildenafil kunye ne-vardenafil.Ifakwe ngokukhawuleza kwaye iphakame ekugxininiseni (378 μg / L emva kwe-dose ye-20-mg) emva kweeyure ze-2, ibonisa isiqingatha sobomi beeyure ze-17.5.Kwakhona i-metabolized yisibindi (CYP3A4).Ngokucacileyo, i-pharmacokinetics yayo ayichaphazeli ngokwezonyango kutywala okanye ukutya okanye izinto ezifana nesifo seswekile okanye ukungasebenzi kakuhle kwesibindi okanye izintso.

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