Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Drug Metabolism & Disposition
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Drug Metabolism & Disposition

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Visit dmd on Facebook
  • Follow dmd on Twitter
  • Follow ASPET on LinkedIn
Abstract

Enantioselective hydrolysis of lorazepam 3-acetate by esterases in human and rat liver microsomes and rat brain S9 fraction.

K Liu, F P Guengerich and S K Yang
Drug Metabolism and Disposition May 1991, 19 (3) 609-613;
K Liu
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
F P Guengerich
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
S K Yang
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

Rates of hydrolysis of racemic and enantiomeric lorazepam 3-acetates (LZA) by esterases in human and rat liver microsomes and rat brain S9 fraction were compared. LZA and its hydrolysis product were analyzed by chiral stationary phase HPLC. When rac-LZA was the substrate, the (R)-LZA was hydrolyzed 2.7-fold and 6.8-fold faster than the (S)-LZA by esterases in rat and human liver microsomes, respectively. In contrast, esterases in rat brain S9 fraction were enantioselective toward the (S)-LZA. The specific activities (nmol of LZA hydrolyzed/mg protein/min) of liver microsomes in the hydrolysis of enantiomerically pure (R)-LZA were approximately 210 (rat) and 1330 (human), and in the hydrolysis of enantiomerically pure (S)-LZA were 25 (rat) and 8 (human). The specific activities of rat brain S9 fraction in the hydrolysis of enantiomerically pure (R)-LZA and (S)-LZA were approximately 3 and 6 nmol/mg protein/min, respectively. Results also indicated an enantiomeric interaction in the hydrolysis of rac-LZA; the presence of (R)-LZA stimulated the hydrolysis of (S)-LZA by all esterase preparations, whereas the presence of (S)-LZA stimulated the hydrolysis of (R)-LZA in rat brain S9 fraction and inhibited the hydrolysis of (R)-LZA in rat and human liver microsomes.

 

DMD articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Drug Metabolism and Disposition
Vol. 19, Issue 3
1 May 1991
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • Editorial Board (PDF)
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Drug Metabolism & Disposition article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Enantioselective hydrolysis of lorazepam 3-acetate by esterases in human and rat liver microsomes and rat brain S9 fraction.
(Your Name) has forwarded a page to you from Drug Metabolism & Disposition
(Your Name) thought you would be interested in this article in Drug Metabolism & Disposition.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Abstract

Enantioselective hydrolysis of lorazepam 3-acetate by esterases in human and rat liver microsomes and rat brain S9 fraction.

K Liu, F P Guengerich and S K Yang
Drug Metabolism and Disposition May 1, 1991, 19 (3) 609-613;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero

Share
Abstract

Enantioselective hydrolysis of lorazepam 3-acetate by esterases in human and rat liver microsomes and rat brain S9 fraction.

K Liu, F P Guengerich and S K Yang
Drug Metabolism and Disposition May 1, 1991, 19 (3) 609-613;
del.icio.us logo Digg logo Reddit logo Twitter logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About DMD
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Journal of Pharmacology and Experimental Therapeutics
  • Molecular Pharmacology
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-009X (Online)

Copyright © 2022 by the American Society for Pharmacology and Experimental Therapeutics