바데나필

한글명:바데나필

카스 번호224785-91-5

상품명:Vardenafil hydrochloride

CBNumberCB6672278

분자식C23H33ClN6O4S

포뮬러 무게525.07

MOL 파일224785-91-5.mol

동의어(한글)

바데나필

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화학적 성질

녹는점	214-216°C
저장 조건	Store at -20°C
용해도	DMSO: 100 mg/mL (190.45 mM); Water: ≥ 100 mg/mL (190.45 mM)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 미색까지의 결정질
InChIKey	XCMULUAPJXCOHI-UHFFFAOYSA-N
SMILES	C(C1=NC(C)=C2C(N=C(C3C=C(S(N4CCN(CC)CC4)(=O)=O)C=CC=3OCC)NN12)=O)CC.Cl

위험 및 안전 성명

HS 번호

2933299090

그림문자(GHS)

바데나필 화학적 특성, 용도, 생산

개요
Vardenafil was the second agent to be marketed and had the advantage that its onset time was not reduced by taking the medication on a full stomach . It is 30 times more potent as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil, with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4 and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000 nM.
화학적 성질
White to Off-White Cyrstalline Solid
용도
vardenafil hydrochloride is a selective phsphodiesterase type 5 (pde5) inhibitor that is used as a urological agent in the treatment of erectile dysfunction.
일반 설명
Vardenafil, 4-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one(Levitra), was the second PDE5 introduced in the U.S. market.The metabolism of vardenafil is primarily by CYP3A4.As such, concomitant use of CYP3A4 inhibitors such as ritonavir,indinavir, ketoconazole, as well as moderate CYP3Ainhibitors such as erythromycin typically results in significantincreases of plasma levels of vardenafil.
효소 저해제
Vardenafil also is rapidly absorbed and peaks in concentration (9.05 μg/mL after a 10-mg dose) after 0.9 hours, displaying a half-life of 4 to 5 hours. The absorption rate of both sildenafil and vardenafil are reduced when taken with a high-fat diet. The drug also is metabolized by hepatic CYP3A4, and a potential for drug–drug interaction with inhibitors or enhancers of CYP3A4 exists. Biochemical studies demonstrate a significant increase in selectivity of vardenafil over sildenafil for PDE5 versus PDE6. Whether this translates into a significant improvement in side effects must await studies in a greater population of patients.

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