PharmPK Discussion - Benztropine

• On 24 Jul 2007 at 08:45:38, "Nagaraju Poola" (poolan.aaa.wyeth.com) sent the message
  

  
  Dear PK Group Members,
  
  Is Benztropine a substrate for any CYPs?
  
  Any reference will be useful.
  
  Thank you in advance.
  
  

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• On 24 Jul 2007 at 11:34:27, "Ahmed Othman" (aothm001.-at-.umaryland.edu) sent the message
  

  
  Hi Nagaraju,
  Benztropine and its analogs are mainly substrates for human CYP2D6
  and CYP2C19 and for rat CYP2C11. Please find below a reference for a
  study that we conducted with the benztropine analog 4',4''-diCl BZT.
  Hope that will help..
  Othman et al., "Transport, metabolism, and in vivo population
  pharmacokinetics of the chloro benztropine analogs, a class of
  compounds extensively evaluated in animal models of drug abuse", The
  Journal of Pharmacology and Experimental Therapeutics. 2007, 320 (1):
  344- 353
  Ahmed
  
  --
  Ahmed Abdel-Fattah Othman
  Ph.D. Candidate
  Pharmacokinetics and Biopharmaceutics lab
  School of Pharmacy
  University of Maryland at Baltimore
  20 Penn Street,HSF-2
  Baltimore, MD 21201
  Phone:(410)706-7388
  E-Mail:- aothm001.at.umaryland.edu
  
  

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• On 24 Jul 2007 at 11:47:18, ArmenP.-a-.aol.com sent the message
  

  
  Dr. Poola:
  
  An examination of the chemical structure of benztropine will give
  potential metabolic pathways.  There is most likely N-oxidation and N-
  demethylation.  In addition hydroxylation of the phenyl rings
  (probably in the 4-position) is also likely.  The metabolic products
  should be formed by these 3 individual reactions or combinations of
  the three.  All of these pathways will involve CYP:  probably 2D6 and
  3A4.  For the hydroxylated metabolites, Phase II glucuronates can be
  expected.
  
  Armen Melikian
  Drug Metabolism Resources
  
  

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