Article
In vitro inhibition and enhancement of liver microsomal S-777469 metabolism by long-chain fatty acids and serum albumin: insight into in vitro and in vivo discrepancy of metabolite formation in humans.
Xenobiotica; the fate of foreign compounds in biological systems - 1 Jan 2016
Sekiguchi Kazutaka, Kanazu Takushi, Murayama Norie, Yamazaki Hiroshi, Yamaguchi Yoshitaka
Abstract excerpt
1. It was previously demonstrated that 10% of S-777469, a cannabinoid receptor 2 selective agonist, is metabolized to its carboxylic acid metabolite (S-777469 5-carboxylic acid, 5-CA) in humans in vivo, while the formation of 5-CA is extremely low in human cryopreserved hepatocytes and liver microsomes (HLMs). In this study, factors causing the different metabolite formation rates of S-777469 in vitro and in vivo...
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