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【答案】应助回帖
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感谢参与，应助指数 +1
1006939364(心静_依然代发): 金币+40, 感谢应助 2015-05-24 10:07:20
默克
Tadalafil
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Monograph ID: M10427 Title: Tadalafil CAS Registry Number: 171596-29-5 CAS Name: (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1′,2′:1,6]‐pyrido[3,4-b]indole-1,4-dione Additional Names: (6R,12aR)-2,3,6,7,12,12a-hexahydro-2-methyl-6-[3,4-(methylenedioxy)phenyl]pyrazino[1′,2′:1,6]‐pyrido[3,4-b]indole-1,4-dione Manufacturer Code: GF-196960; IC-351 Trademark Names: Adcirca (Lilly); Cialis (Lilly) Molecular Formula: C22H19N3O4 Molecular Weight: 389.41 Percent Composition: C 67.86%, H 4.92%, N 10.79%, O 16.43% Standard InChI: InChI=1S/C22H19N3O4/c1-24-10-19(26)25-16(22(24)27)9-14-13-4-2-3-5-15(13)23-20(14)21(25)12-6-7-17-18(8-12)29-11-28-17/h2-8,16,21,23H,9-11H2,1H3/t16-,21-/m1/s1Copy Copied Standard InChIKey: WOXKDUGGOYFFRN-IIBYNOLFSA-NCopy Copied Properties
White crystals from 2-propanol, mp 302-303 °C. [α]D20 +71.0 (c = 1.00 in CHCl3). Very slightly sol in ethanol. Practically insol in water.
References
Selective type 5 cGMP phosphodiesterase (PDE-5) inhibitor. Prepn: A. C. Daugan, WO 9519978 (1995 to Glaxo); eidem, US 5859006 (1999 to ICOS); and PDE-5 inhibition: idem et al., J. Med. Chem. 46, 4525, 4533 (2003) DOI: 10.1021/jm030056e PMID: 14521414. HPLC determn in plasma: C.-L. Cheng, C.-H. Chou, J. Chromatogr. B 822, 278 (2005) DOI: 10.1016/j.jchromb.2005.06.017. Clinical pharmacokinetics: S. T. Forgue et al., Br. J. Clin. Pharmacol. 61, 280 (2005) DOI: 10.1111/j.1365-2125.2005.02553.x PMID: 16487221. Clinical comparison with sildenafil for erectile disfunction: I. Eardley et al., BJU Int. 96, 1323 (2005) DOI: 10.1111/j.1464-410X.2005.05892.x PMID: 16287454. Clinical trial in pulmonary arterial hypertension: N. Galié et al., Circulation 119, 2894 (2009) DOI: 10.1161/CIRCULATIONAHA.108.839274 PMID: 19470885. Review of cardiovascular effects: T. Reffelmann et al., Expert Opin. Drug Saf. 7, 43-52 (2008) DOI: 10.1517/14740338.7.1.43 PMID: 18171313.
Classifications
Therapeutic Category: Erectile Dysfunction Treatment; Phosphodiesterase Inhibitor; Pulmonary Hypertension Treatment
Keywords: In treatment of male erectile dysfunction. In treatment of pulmonary arterial hypertension.
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