Imepitoin
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| Clinical data | |
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| Trade names | Pexion |
| Other names | AWD 131-138; ELB-138 |
| Routes of administration | Oral |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.220.751 |
| Chemical and physical data | |
| Formula | C13H14ClN3O2 |
| Molar mass | 279.72 g·mol−1 |
| 3D model (JSmol) | |
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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]
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]
See also
[edit]References
[edit]- ^ a b c d e f Rundfeldt C, Löscher W (2014). "The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy". CNS Drugs. 28 (1): 29–43. doi:10.1007/s40263-013-0129-z. PMID 24357084. S2CID 31627280.
- ^ a b c d Sanders S (29 April 2015). "Antiseizure Medications". Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN 978-1-118-68970-7.
- ^ a b c Thomas WB, Dewey CW (8 September 2015). "Seizures and Narcolepsy". In Dewey CW, da Costa RC (eds.). Practical Guide to Canine and Feline Neurology. Wiley. p. 259. ISBN 978-1-119-06204-2.
- ^ a b "Imepitoin". drugs.com. Archived from the original on 2019-06-17. Retrieved 2017-09-17.
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