| Identification | Back Directory | [Name]
2-(2-CHLOROPHENYL)-2-HYDROXYETHYL CARBAMATE | [CAS]
194085-75-1 | [Synonyms]
YKP 509
RWJ 333369
Carisbamate
JNJ 10234094
(S)-Carisbamate
CarisbaMate (RWJ-333369)
2-(2-CHLOROPHENYL)-2-HYDROXYETHYL CARBAMATE
[(2S)-2-(2-chlorophenyl)-2-hydroxyethyl] carbamate
1,2-ETHANEDIOL,1-(2-CHLOROPHENYL)-, 2-CARBAMATE, (S)-
1,2-Ethanediol,1-(2-chlorophenyl)-, 2-carbaMate, (1S)- | [Molecular Formula]
C813CH8D2Cl15NO3 | [MDL Number]
MFCD15071195 | [MOL File]
194085-75-1.mol | [Molecular Weight]
215.63 |
| Chemical Properties | Back Directory | [Melting point ]
131-132°C | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
White to Off-White | [Optical Rotation]
[α]/D +77 to +87°, c =0.2 in chloroform-d |
| Hazard Information | Back Directory | [Description]
Carisbamate is an antiepileptic agent., In vivo, administration of carisbamate (10-60 mg/kg) dose-dependently reduces spike and wave discharges in the frontoparietal cortex in a rat model of absence seizures. Carisbamate (10 mg/kg) increases latency to the first running episode in the Wistar audiogenic sensitive rat model of convulsive seizures. It also reduces motor seizure frequency in a rat model of spontaneous seizures in a dose-dependent manner. Carisbamate blocks Nav1.2 channels (IC50 = 68 μM for rat channels) and inhibits repetitive firing of action potentials in rat hippocampal neurons in a dose-dependent manner. It also reduces T-type Ca2+ currents in HEK cells transfected with human recombinant Cav3.1 channels at a concentration of 300 μM. | [Uses]
Carisbamate is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizure models, an
d exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models. | [Uses]
Carisbamate is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizure models, and exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models. | [Uses]
Labelled Carisbamate; it is being developed for adjuvant treatment of partial onset epilepsy. Carisbamate produces anticonvulsant effects in primary generalized, complex partial and absence-type seizu
re models, and exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models. | [Definition]
ChEBI: Carisbamate is an organochlorine compound. | [in vivo]
Carisbamate (10, 30, 60 mg/kg; i.p.; single) dose dependently reduces the expression of spike-and-wave discharges (SWD) in absence seizures rat model[2].
Carisbamate (20, 30 mg/kg; i.p.; single) shows no wild running episode or tonic seizure occurres in any of the rats tested[2]. | Animal Model: | Male genetic absence epilepsy rat (absence seizures model)[2]. | | Dosage: | 10, 30, 60 mg/kg | | Administration: | Intraperitoneal injection; single. | | Result: | Completely inhibited SWD when at 60 mg/kg after 120 min, and restored the duration of SWD to the control level when at 30 mg/kg after 100 min. |
| Animal Model: | Male Wistar audiogenic sensitive rat (convulsive seizures model)[2]. | | Dosage: | 10, 20, 30 mg/kg | | Administration: | Intraperitoneal injection; single. | | Result: | Showed no wild running episode or tonic seizure occurred in any of the rats tested when at 20 and 30 mg/kg.
Increased by 327% the latency to the tonic seizure that still occurred in the six of eight rats studied when at 10 mg/kg.
|
| [storage]
Store at -20°C | [References]
[1] JENNIFER FRAN?OIS Astrid N Any Boehrer. Effects of Carisbamate (RWJ-333369) in Two Models of Genetically Determined Generalized Epilepsy, the GAERS and the Audiogenic Wistar AS[J]. Epilepsia, 2007, 49 3: 393-399. DOI: 10.1111/j.1528-1167.2007.01278.x
[2] HEIDI L. GRABENSTATTER F. E D. A new potential AED, carisbamate, substantially reduces spontaneous motor seizures in rats with kainate-induced epilepsy[J]. Epilepsia, 2008, 49 10: 1787-1794. DOI: 10.1111/j.1528-1167.2008.01657.x
[3] YI LIU . Carisbamate, a novel neuromodulator, inhibits voltage-gated sodium channels and action potential firing of rat hippocampal neurons[J]. Epilepsy Research, 2009, 83 1: Pages 66-72. DOI: 10.1016/j.eplepsyres.2008.09.006
[4] DO YOUNG KIM. Carisbamate blockade of T-type voltage-gated calcium channels[J]. Epilepsia, 2017, 58 4: 617-626. DOI: 10.1111/epi.13710 |
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