Imepitoin

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Imepitoin
Imepitoin.svg
Clinical data
Trade namesPexion
Other namesAWD 131-138; ELB-138
Routes of
administration
Oral
ATCvet code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.220.751 Edit this at Wikidata
Chemical and physical data
FormulaC13H14ClN3O2
Molar mass279.72 g·mol−1
3D model (JSmol)

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 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]

  1. ^ 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.
  2. ^ a b c d Sean Sanders (29 April 2015). Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN 978-1-118-68970-7.
  3. ^ a b c Curtis W. Dewey; Ronaldo C. da Costa (8 September 2015). Practical Guide to Canine and Feline Neurology. Wiley. pp. 806–. ISBN 978-1-119-06204-2.
  4. ^ a b https://www.drugs.com/international/imepitoin.html