Imepitoin (INN ), sold under the brand name Pexion, is an anticonvulsant which is used in veterinary medicine in Europe to treat epilepsy in dogs.[1][2][3][4] It was recently[when?] approved in the United States.[2][3][4] The drug also has anxiolytic effects.[1][2] 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.[1][2]
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Trade names | Pexion |
Other names | AWD 131-138; ELB-138 |
Routes of administration | Oral |
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ECHA InfoCard | 100.220.751 |
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Formula | C13H14ClN3O2 |
Molar mass | 279.72 g·mol−1 |
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Imepitoin acts as a low-affinity (4,350–5,140 nM; relative to Ki = 6.8 nM for diazepam and Ki = 1.7 nM for clonazepam) partial agonist of the benzodiazepine site of the GABAA receptor (up to 12–21% of the maximal potentiation of diazepam, a full agonist of this site).[1] It is the first partial agonist to be approved for the treatment of epilepsy.[1] The drug also dose-dependently blocks voltage-gated calcium channels.[3] It is not a benzodiazepine; instead, it is an imidazolone, and bears some structural similarities to hydantoin anticonvulsants like ethotoin and phenytoin.[1]