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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 |
| Chemical and physical data | |
| Formula | C13H14ClN3O2 |
| Molar mass | 279.72 g·mol−1 |
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Imepitoin (INNTooltip International Nonproprietary Name), sold under the brand namePexion, is ananticonvulsant which is used inveterinary medicine inEurope to treatepilepsy in dogs.[1][2][3][4] It was recently[when?] approved in theUnited States.[2][3][4] The drug also hasanxiolytic effects.[1][2] It was originally developed to treat epilepsy in humans, butclinical trials were terminated upon findings of unfavorablemetabolic differences insmokers and non-smokers.[1][2]
Imepitoin acts as a low-affinity (4,350–5,140 nM; relative to Ki = 6.8 nM fordiazepam and Ki = 1.7 nM forclonazepam)partial agonist of thebenzodiazepine site of theGABAA receptor (up to 12–21% of the maximal potentiation of diazepam, afull agonist of this site).[1] It is the firstpartial agonist to be approved for the treatment of epilepsy.[1] The drug also dose-dependentlyblocksvoltage-gated calcium channels.[3] It isnot a benzodiazepine; instead, it is animidazolone, and bears somestructuralsimilarities tohydantoin anticonvulsants likeethotoin andphenytoin.[1]
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