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Imepitoin

Imepitoin (), sold under the brand name Pexion, is an anticonvulsant which is used in veterinary medicine in Europe to treat epilepsy in dogs. It was approved in the United States for veterinary use in December 2018. The drug also has anxiolytic effects. It was originally developed to treat epilepsy in humans, but clinical trials were terminated upon findings of unfavorable metabolic differences in smokers and non-smokers.

Imepitoin acts as a low-affinity (4,350–5,140&nbsp;nM; relative to K<sub>i</sub> = 6.8&nbsp;nM for diazepam and K<sub>i</sub> = 1.7&nbsp;nM for clonazepam) partial agonist of the benzodiazepine site of the GABA<sub>A</sub> receptor (up to 12–21% of the maximal potentiation of diazepam, a full agonist of this site). It is the first partial agonist to be approved for the treatment of epilepsy. The drug also dose-dependently blocks voltage-gated calcium channels. It is not a benzodiazepine; instead, it is an imidazolone, and bears some structural similarities to hydantoin anticonvulsants like ethotoin and phenytoin.

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