Stereochemistry | ACHIRAL |
Molecular Formula | C13H14ClN3O2 |
Molecular Weight | 279.722 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C(C=C1)N2CC(=NC2=O)N3CCOCC3
InChI
InChIKey=IQHYCZKIFIHTAI-UHFFFAOYSA-N
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
Molecular Formula | C13H14ClN3O2 |
Molecular Weight | 279.722 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Imepitoin (AWD 131–138 or ELB 138; 1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one) is a new anti-epileptic drug recently approved in the European Union for the treatment of canine idiopathic epilepsy. It was developed from a series of imidazolinones due to its pronounced ant seizure activity in a large variety of rodent models of epileptic seizures, combined with a high tolerability in these models. Imepitoin is a centrally acting antiepileptic substance, which crosses the blood brain barrier without involvement of active transport or active clearance, resulting in immediate equilibrium between plasma and brain. Imepitoin acts as low-affinity partial agonists at the benzodiazepine (BZD) site of the GABAA receptor. Hopefully, that the favorable profile of imepitoin for the treatment of epilepsy in dogs will reactivate the interest in partial BZD site agonists as new treatments for human epilepsy.
CNS Activity
Approval Year
PubMed
Patents
Sample Use Guides
for dog:
Oral administration at a dose range of 10 mg to 30 mg imepitoin per kg body weight twice daily, approximately 12 hours apart. Each tablet can be halved for appropriate dosing according to the individual body weight of the dog. The required dose will vary between dogs and will depend on the severity of the disorder. The recommended initial dose of imepitoin is 10 mg per kg body weight twice daily.
Initiate therapy using the bodyweight in kg and the dosing table. If seizures are not adequatey reduced
following a minimum of 1 week of treatment at the current dose the supervising veterinary surgeon
should re-assess the dog. Assuming that the veterinary medicinal product is well tolerated by the dog,
the dose can be increased by 50 to 100% increments up to a maximum dosage of 30 mg per kg
administered twice daily.
Route of Administration:
Oral