Imepitoin (), sold under the brand name Pexion, is an

anticonvulsant Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...

which is used in veterinary medicine in Europe to treat epilepsy in dogs.
/ref> It was recently approved in the United States. The drug also has anxiolytic effects. It was originally developed to treat epilepsy in humans, but clinical trials were terminated upon findings of unfavorable

metabolic Metabolism (, from el, μεταβολή ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cell ...

differences in smokers and non-smokers. Imepitoin acts as a low-

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Partn ...

(4,350–5,140 nM; relative to K_i = 6.8 nM for diazepam and K_i = 1.7 nM for clonazepam) partial agonist of the

benzodiazepine site The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on ...

of the GABA_A receptor (up to 12–21% of the maximal potentiation of diazepam, a full agonist of this site). It is the first partial agonist to be approved for the treatment of epilepsy. The drug also dose-dependently blocks

voltage-gated calcium channel Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'', muscle, glial cells, neurons, etc.) with a permeabi ...

s. It is not a benzodiazepine; instead, it is an

imidazolone Imidazolones are a family of heterocyclic compounds, the parents of which have the formula OC(NH)2(CH)2. Two isomers are possible, depending on the location of the carbonyl (CO) group. The NH groups are nonadjacent. A common route to imidazol-2 ...

, and bears some structural similarities to

hydantoin Hydantoin, or glycolylurea, is a heterocyclic organic compound with the formula CH2C(O)NHC(O)NH. It is a colorless solid that arises from the reaction of glycolic acid and urea. It is an oxidized derivative of imidazolidine. In a more general sen ...

anticonvulsants like

ethotoin Ethotoin (previously marketed as Peganone) is an anticonvulsant drug used in the treatment of epilepsy. It is a hydantoin, similar to phenytoin. It is not available in the United States. Mechanism of action Similar to phenytoin. Approval hi ...

and phenytoin.

References

Anticonvulsants Anxiolytics Calcium channel blockers Chloroarenes GABAA receptor positive allosteric modulators 4-Morpholinyl compunds Veterinary drugs {{anticonvulsant-stub

See also

References