Centchroman: in vitro metabolism by rat liver homogenate

Ratna, Sanjeev ; Roy, S. K. ; Ray, Suprabhat ; Kole, P. L. ; Salman, M. ; Madhusudan, K. P. ; Sircar, K. P. ; Anand, N. (1986) Centchroman: in vitro metabolism by rat liver homogenate Drug Development Research, 7 (2). pp. 173-178. ISSN 0272-4391

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Official URL: http://www3.interscience.wiley.com/journal/1096705...

Related URL: http://dx.doi.org/10.1002/ddr.430070208


Centchroman (trans-2,2-dimethyl-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman) (I), a postcoital antifertility agent under clinical development was extensively metabolized by rat liver homogenate in vitro. Employing field desorption mass spectrometry, high performance liquid chromatography, comparison with authentic samples, and studies with 2-14C-Centchroman, seven metabolites have so far been characterised, which include trans-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman (II, 37.5%), trans-2,2-dimethyl-3-phenyl-4-(p-(β pyrrolidinoethoxy) phenyl)-7-hydroxy chroman (III, 2.5%), β pyrrolidino-ethoxy benzene (IV), 2,2-dimethyl-4-(p-(hydroxy) phenyl)-7-methoxy chromene (V, 39.4%), trans-2,2-dimethyl-3-phenyl-4-(p-(hydroxy) phenyl)-7-methoxy chroman (VI, 5.8%), 2,3-trans-3,4-trans-2-methyl-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chorman (VII, 2.9%), and 2,2-dimethyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman (VIII, 8.8%). Formation of metabolites V and VIII are unusual cases of dephenylation during metabolism.

Item Type:Article
Source:Copyright of this article belongs to John Wiley and Sons, Inc.
Keywords:Antifertilitic Agent; Centchroman; Metabolism
ID Code:3817
Deposited On:18 Oct 2010 09:42
Last Modified:12 May 2011 06:54

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