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Metabolism of dicentrine: identification of the phase I and phase II metabolites in miniature pig urine.
MedLine Citation:
PMID:  20622045     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
The metabolic profile of dicentrine, a selective α(1)-adrenoceptor antagonist with potent antiarrhythmic and antihypertensive activities, in miniature pig urine via oral administration was investigated for the first time. The urine, collected after a single oral administration of dicentrine, was pretreated using solvent extraction and column chromatographic methods to identify the metabolites containing fractions. Twenty-four metabolites (MI-1-9 and MII-1-15), of which 21 compounds are new, were identified by mass spectrometry and high-performance liquid chromatography-diode array detector solid-phase extraction-NMR techniques. Of these, 14 metabolites (MI-5, MII-1 and 2, and MII-5-15) were further isolated for structure confirmation. The phase I metabolic transformations of dicentrine were found to be N-demethylation, N-oxidation, O-demethylation (9,10-OMe), O,O-demethylenation (1-OCH(2)O-2), and hydroxylation at the benzylic (C-4) and the aromatic (C-3) positions, whereas those for the phase II were O-glucuronidation and O-glucosylation of the phenolic group of the phase I metabolites.
Authors:
Yi-Chun Lai; Tzong-Fu Kuo; Chien-Kuang Chen; Han-Ju Tsai; Shoei-Sheng Lee
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-07-09
Journal Detail:
Title:  Drug metabolism and disposition: the biological fate of chemicals     Volume:  38     ISSN:  1521-009X     ISO Abbreviation:  Drug Metab. Dispos.     Publication Date:  2010 Oct 
Date Detail:
Created Date:  2010-09-21     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9421550     Medline TA:  Drug Metab Dispos     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1714-22     Citation Subset:  IM    
Affiliation:
School of Pharmacy, College of Medicine, National Taiwan University, 1 Sec. 1 Jen-Ai Rd., Taipei, Taiwan, R.O.C.
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