Determination of a New Type of Phosphodiesterase-5 Inhibitor, Thioquinapiperifil, in a Dietary Supplement Promoted for Sexual Enhancement

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概要

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• A new type of phosphodiesterase-5 (PDE-5) inhibitor, thioquinapiperifil (1), was found in dietary supplements. LC-MS analysis indicated that the supplements contain two major compounds. One was identified as thiodenafil (synonym: thiosildenafil) by direct comparison with the authentic compound. The other showed a molecular weight of 448, and accurate mass measurement showed its elemental composition to be C_<24>H_<28>N_6O_1S_1.Together, the mass and NMR spectrometric data revealed that the compound is an imidazoquinazoline derivative: 3-ethyl-1, 3-dihydro-8-[[[2-[4-(hydroxymethyl)-1-piperidinyl]phenyl]methyl]amino]-2H-imidazo[4, 5-g] quinazoline-2-thione. This compound had been synthesized as a PDE-5 inhibitor, formerly reported as KF31327 by Kyowa Hakko Kogyo Co., Ltd. Considering this compound's general properties, it has been renamed thioquinapiperifil with the agreement of Kyowa Hakko Kogyo Co., Ltd. The detection of imidazoquinazoline-type compounds in dietary supplements has not been reported. Quantitative analysis showed that the contents of 1 and thiodenafil in the products were about 13-15mg/tablet (43-48μg/mg) and about 0.4mg/tablet (1μg/mg), respectively.

• 公益社団法人日本薬学会の論文
• 2008-09-01

著者

• GODA Yukihiro

  National Institute of Health Sciences

• HAISHIMA Yuji

  National Institute of Health Sciences

• Uchiyama N

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Uchiyama Nahoko

  National Institute Of Health Sciences

• Goda Yukihiro

  National Inst. Of Health Sciences

• Guo Yahong

  Graduate School Of Pharmaceutical Sciences Nagoya City University

• Kikura-hanajiri Ruri

  National Institute Of Health Sciences

• SAISHO Kazuhiro

  National Institute of Health Sciences

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