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Imepitoin
Clinical data
Trade namesPexion
Other namesAWD 131-138; ELB-138
Routes of
administration		 Oral
ATCvet code
Identifiers
  • 3-(4-Chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard ( EPA)
ECHA InfoCard 100.220.751 Edit this at Wikidata
Chemical and physical data
FormulaC13H14ClN3O2
Molar mass279.72 g·mol−1
3D model ( JSmol)
  • C1COCCN1C2=NC(=O)N(C2)C3=CC=C(C=C3)Cl
  • InChI=1S/C13H14ClN3O2/c14-10-1-3-11(4-2-10)17-9-12(15-13(17)18)16-5-7-19-8-6-16/h1-4H,5-9H2
  • Key:IQHYCZKIFIHTAI-UHFFFAOYSA-N

Imepitoin ( INNTooltip International Nonproprietary Name), 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

References

  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 Sanders S (29 April 2015). "Antiseizure Medications". Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN  978-1-118-68970-7.
  3. ^ 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.
  4. ^ a b "Imepitoin". drugs.com. Archived from the original on 2019-06-17. Retrieved 2017-09-17.


Stub icon

This anticonvulsant-related article is a stub. You can help Wikipedia by expanding it.

Retrieved from " https://en.wikipedia.org/?title=Imepitoin&oldid=1191560993"
From Wikipedia, the free encyclopedia
Imepitoin
Clinical data
Trade namesPexion
Other namesAWD 131-138; ELB-138
Routes of
administration		 Oral
ATCvet code
Identifiers
  • 3-(4-Chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard ( EPA)
ECHA InfoCard 100.220.751 Edit this at Wikidata
Chemical and physical data
FormulaC13H14ClN3O2
Molar mass279.72 g·mol−1
3D model ( JSmol)
  • C1COCCN1C2=NC(=O)N(C2)C3=CC=C(C=C3)Cl
  • InChI=1S/C13H14ClN3O2/c14-10-1-3-11(4-2-10)17-9-12(15-13(17)18)16-5-7-19-8-6-16/h1-4H,5-9H2
  • Key:IQHYCZKIFIHTAI-UHFFFAOYSA-N

Imepitoin ( INNTooltip International Nonproprietary Name), 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

References

  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 Sanders S (29 April 2015). "Antiseizure Medications". Seizures in Dogs and Cats. Wiley. pp. 209–. ISBN  978-1-118-68970-7.
  3. ^ 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.
  4. ^ a b "Imepitoin". drugs.com. Archived from the original on 2019-06-17. Retrieved 2017-09-17.


Stub icon

This anticonvulsant-related article is a stub. You can help Wikipedia by expanding it.

Retrieved from " https://en.wikipedia.org/?title=Imepitoin&oldid=1191560993"

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