Abstract
The metabolism of probenecid in vitro was investigated with rat, mouse, and human liver preparations. As in previous in vivo studies, metabolism in vitro was found to be limited to the side chain. This metabolism involved mono-N-depropylation and hydroxylation in the 2- and 3-positions (3-hydroxy probenecid was in part converted to the carboxy metabolite). Acyl glucuronide conjugation was minimal. The presence of multiple forms of microsomal oxidative enzymes was suggested by the effects of: a) phenobarbital pretreatment, b) drug-metabolizing enzyme inhibitors, and c) variations in ionic strength and buffer composition on the metabolism of probenecid.
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.
|
Log in using your username and 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.