Abstract:
:Metabotropic glutamate receptors (mGluR) are G-protein-coupled receptors that play a major role in modulatory pathways in the CNS and have been suggested to have pharmacological implications in pain, psychiatric disorders and other neurological states. 3-[(2-Methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP) is a specific and selective antagonist for the mGluR sub-type 5. Previous studies using rat liver microsomes showed that the major oxidative metabolites of MTEP are a hydroxymethyl metabolite (M1), two oxides (M2 and M4), a thiazole-ring opened metabolite (M3) and CO(2) (M5). In the present study, we examined the metabolism of MTEP in liver microsomes and expressed rat and human CYP isoforms. In rat liver microsomes, metabolic stability studies accurately predicted the in vivo clearance for MTEP. Incubation of MTEP with expressed rat and human CYP isoforms showed that CYP1A and CYP2C isoforms are primarily responsible for the metabolism of this compound. The results suggest that species differences in MTEP metabolism is possible and could contribute to specie-differences in biological effects of the compound.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Green MD,Yang X,Cramer M,King CDdoi
10.1016/j.neulet.2005.08.032keywords:
subject
Has Abstractpub_date
2006-01-02 00:00:00pages
91-5issue
3eissn
0304-3940issn
1872-7972pii
S0304-3940(05)00957-2journal_volume
391pub_type
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