Identification of rat faecal, urinary and biliary metabolites of thionorphine, a novel mixed agonist‐antagonist analgesic, using liquid chromatography/electrospray ionization tandem mass spectrometry | Zendy

Wei Shuxiang | Zendy; Zhang Zhenqing | Zendy; Wang Xiaoying | Zendy; Guo Jifen | Zendy

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Identification of rat faecal, urinary and biliary metabolites of thionorphine, a novel mixed agonist‐antagonist analgesic, using liquid chromatography/electrospray ionization tandem mass spectrometry

Author(s) -

Wei Shuxiang,

Zhang Zhenqing,

Wang Xiaoying,

Guo Jifen

Publication year - 2004

Publication title -

biopharmaceutics and drug disposition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.419

H-Index - 58

eISSN - 1099-081X

pISSN - 0142-2782

DOI - 10.1002/bdd.360

Subject(s) - chemistry , chromatography , analgesic , electrospray ionization , tandem mass spectrometry , mass spectrometry , liquid chromatography–mass spectrometry , antagonist , agonist , urinary system , electrospray , pharmacology , endocrinology , biochemistry , medicine , receptor

The biotransformation of thionorphine (N‐cyclopropylmethyl‐7α‐[(s)‐1‐hydroxy‐1‐methyl‐3‐(2thiophene)‐propyl]‐6,14‐endo‐ethano tetrahydrooripavine), a new analgesic, was in‐vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ion mode, in which a mobile phase of 10mM ammonium acetate (pH 3.0)/acetonitrile (25/75) was used, suggested that thionorphine is biotransformed to two potentially active metabolites, the N‐dealkylated thionorphine (M‐I) and the oxidized thionorphine (M‐II), and subsequently form conjugates with glucuronic acid of both thionorphine and the metabolites. Copyright © 2004 John Wiley & Sons, Ltd.

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