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Dear readers,
When using commercially available or self-prepared rat liver microsomes
for metabolic studies on novel chemical entities for which there are no
previously reported metabolic studies, what type of positive control
would you recommend that one could/should use to confirm that the
microsomes are indeed working?
Is there any compound that is best metabolized by just any uninduced
batch of rat liver microsomes (in incubation with all the necessary
coenzymes), that one could use as positive control in such studies?
Thanks for any suggetions.
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Dear Natalie,
We have been using two compounds, propranolol and alprazolam, as
positive controls for metabolic stability studies in drug discovery
projects. These two compounds cover 2C19, 2D6 and 3A4. When you
consider how many controls you want to use, you have to balance
reliability and throughput.
Zhaoyang LI, Ph.D.
Pharmacokinetics and Drug Metabolism
Biogen, Inc.
(617)679-6294
(617)679-2225 (fax)
Zhaoyang_Li.-a-.Biogen.com
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