Art

J-GLOBAL ID：201502247915029331   Reference number：15A0170039

Contribution of CYP3A Isoforms to Dealkylation of PDE5 Inhibitors: A Comparison between Sildenafil N-Demethylation and Tadalafil Demethylenation

PDE5阻害薬の脱アルキル化に対するCYP3Aアイソフォームの関与:シルデナフィルのN-脱メチル化とタダラフィルの脱メチレン化との比較

Author (9)： TAKAHIRO Rikako (Graduate School of Medicine and Pharmaceutical Sciences, Univ. of Toyama) ,  NAKAMURA Saki (Graduate School of Medicine and Pharmaceutical Sciences, Univ. of Toyama) ,  KOHNO Hiroyuki (Graduate School of Medicine and Pharmaceutical Sciences, Univ. of Toyama) ,  YOSHIMURA Naoki (First Dep. of Surgery, Fac. of Medicine, Univ. of Toyama) ,  NAKAMURA Tsuneyuki (Dep. of Pediatrics, Kanazawa Medical Univ.) ,  OZAWA Sayaka (Dep. of Pediatrics, Fac. of Medicine, Univ. of Toyama) ,  HIRONO Keiichi (Dep. of Pediatrics, Fac. of Medicine, Univ. of Toyama) ,  ICHIDA Fukiko (Dep. of Pediatrics, Fac. of Medicine, Univ. of Toyama) ,  TAGUCHI Masato (Graduate School of Medicine and Pharmaceutical Sciences, Univ. of Toyama)
Material： Biological and Pharmaceutical Bulletin  (Biological & Pharmaceutical Bulletin)
Volume： 38  Issue： 1  Page： 58-65 (J-STAGE)  Publication year： 2015 
JST Material Number： S0989A  ISSN： 0918-6158  CODEN： BPBLEO  Document type： Article
Article type： 原著論文  Country of issue： Japan (JPN)  Language： ENGLISH (EN)

Thesaurus term： human ,...
Semi thesaurus term： phosphodiesterase 5 inhibitor ,...

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JST classification (3)： Basic research of drugs acting on urinary system  (GW11010R) ,  Basic biopharmacy  (GY01021U) ,  Enzyme in general  (EB09010D)

Substance index (2)： Sildenafil ,  Tadalafil

Reference (30)：

• 1) Rybalkin SD, Yan C, Bornfeldt KE, Beavo JA. Cyclic GMP phosphodiesterases and regulation of smooth muscle function. Circ. Res., 93, 280-291 (2003).
• 2) Lewis GD, Semigran MJ. Type 5 phosphodiesterase inhibition in heart failure and pulmonary hypertension. Curr. Heart Fail. Rep., 1, 183-189 (2004).
• 3) Takatsuki S, Calderbank M, Ivy DD. Initial experience with tadalafil in pediatric pulmonary arterial hypertension. Pediatr. Cardiol., 33, 683-688 (2012).
• 4) Ghofrani HA, Voswinckel R, Reichenberger F, Olschewski H, Haredza P, Karadas B, Schermuly RT, Weissmann N, Seeger W, Grimminger F. Differences in hemodynamic and oxygenation responses to three different phosphodiesterase-5 inhibitors in patients with pulmonary arterial hypertension: a randomized prospective study. J. Am. Coll. Cardiol., 44, 1488-1496 (2004).
• 5) Nichols DJ, Muirhead GJ, Harness JA. Pharmacokinetics of sildenafil after single oral doses in healthy male subjects: absolute bioavailability, food effects and dose proportionality. Br. J. Clin. Pharmacol., 53 (Suppl. 1), 5S-12S (2002).

Terms in the title (8)： PDE5阻害薬 ,  脱アルキル化 ,  CYP3A ,  アイソフォーム ,  シルデナフィル ,  脱メチル化 ,  タダラフィル ,  メチレン化