Abstract:
:In this study, we describe the effect of antiepileptic drugs on the production of kynurenic acid in rat cortical slices, and on the activity of kynurenic acid biosynthetic enzymes, kynurenine aminotransferases (KATs I and II) in the brain tissue. Phenobarbital, felbamate, phenytoin and lamotrigine (all at 0.5-3.0 mM) enhanced kynurenic acid production in vitro, and stimulated the activity of KAT I. In contrast, vigabatrin, gabapentin and tiagabine inhibited kynurenic acid synthesis in cortical slices with IC(50) of 3.9 (2.8-7.9), 3.7 (2.5-5.4) and 7.5 (3.5-14.3) mM, respectively. Vigabatrin, gabapentin and tiagabine reduced also the activity of KAT I with IC(50) of 1.6 (1.1-2.4), 0.1 (0.01-0.15), 0.9 (0.7-1.2) mM, and the activity of KAT II with IC(50) values of 6.0 (4.8-7.5), 0.2 (0.1-0.3) and 2.0 (1.5-2.6) mM, respectively. In conclusion, the enhancement of kynurenic acid formation displayed by carbamazepine, phenytoin, phenobarbital, felbamate and lamotrigine seems to be a novel mechanism, synergistic with other actions of these drugs, and potentially valuable in terms of better control of epilepsy.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kocki T,Wielosz M,Turski WA,Urbanska EMdoi
10.1016/j.ejphar.2006.05.015subject
Has Abstractpub_date
2006-07-17 00:00:00pages
147-51issue
3eissn
0014-2999issn
1879-0712pii
S0014-2999(06)00503-6journal_volume
541pub_type
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