Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
516.25187436
InChI
InChI=1S/C25H36N6O4S/c1-5-8-20-22-23(31(4)29-20)25(32)28-24(27-22)19-16-18(10-11-21(19)35-15-6-2)36(33,34)26-13-12-17-9-7-14-30(17)3/h10-11,16-17,26H,5-9,12-15H2,1-4H3,(H,27,28,32)
InChI Key
InChIKey=IYFNEFQTYQPVOC-UHFFFAOYSA-N
IUPAC Name
3-{1-methyl-7-oxo-3-propyl-1H,4H,7H-pyrazolo[4,3-d]pyrimidin-5-yl}-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzene-1-sulfonamide
Traditional IUPAC Name
udenafil
SMILES
CCCOC1=C(C=C(C=C1)S(=O)(=O)NCCC1CCCN1C)C1=NC(=O)C2=C(N1)C(CCC)=NN2C
pKa (strongest acidic)
7.21
pKa (Strongest Basic)
8.48
Refractivity
153.11 m3·mol-1
Dược Lực Học :
Udenafil is a potent selective phosphodiesterase type 5 (PDE5) inhibitor.
Cơ Chế Tác Dụng :
Udenafil is a new phosphodiesterase type 5 (PDE5) inhibitor used to treat erectile dysfunction (ED). It has been approved in South Korea and will be marketed under the brand name Zydena. It is not yet approved for use in the U.S., E.U., or Canada.
Udenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by udenafil enhances erectile function by increasing the amount of cGMP.
Dược Động Học :
▧ Metabolism :
Hepatic. Metabolized by CYP3A4 and CYP3A5.
Chỉ Định :
Investigated for use/treatment in erectile dysfunction and hypertension.
Tương Tác Thuốc :
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Isosorbide Dinitrate
The vasodilatory effects of Isosobide dinitrate may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
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Isosorbide Mononitrate
The vasodilatory effects of Isosobide mononitrate may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
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Nitroglycerin
The vasodilatory effects of Nitroglycerin may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
Liều Lượng & Cách Dùng :
Tablet - Oral