| Identification | Back Directory | [Name]
Retigabine Dihydrochloride | [CAS]
150812-13-8 | [Synonyms]
D 20443
Retigabine HCl
Retigabin.2HCl
Retigabine 2HCL
D20443 dihydrochloride
D-20443 dihydrochloride
D 20443 dihydrochloride
Retigabine Dihydrochloride
ethyl 2-aMino-4-(4-fluorobenzylaMino)phenylcarbaMate dihydrochloride
Ethyl [2-amino-4-[[(4-fluorophenyl)methyl]amino]phenyl]carbamate Dihydrochloride
N-(2-Amino-4-(4-fluorobenzylamino)phenyl)carbamic Acid Ethyl Ester Dihydrochloride | [EINECS(EC#)]
2017-001-1 | [Molecular Formula]
C16H20Cl2FN3O2 | [MDL Number]
MFCD00912289 | [MOL File]
150812-13-8.mol | [Molecular Weight]
339.79 |
| Chemical Properties | Back Directory | [Appearance]
Off-White Powder | [Melting point ]
168-170°C | [storage temp. ]
Hygroscopic, -20°C Freezer, Under Inert Atmosphere | [solubility ]
≥18.8 mg/mL in DMSO; ≥52.4 mg/mL in H2O with gentle warming; ≥8.71 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Powder | [Uses]
A new experimental anticonvulsant drug. Anxiolytic. | [Biological Activity]
retigabine is a first-in-class k+ channel (kcnq) opener. kcnq channels are reported to be expressed predominantly in neurons and are critical determinants of cellular excitability, as shown by the occurrence of human genetic mutations in kcnq channels which underlie inheritable disorders including the syndrome of benign familial neonatal convulsions. | [in vitro]
retigabine was found to combine a novel mode of actions, which were namely potassium channel opening (kcnq2, kcnq3 as well as kcnq4 channels). retigabine also showed activities with some potentiation of gamma amino butyric acid (gaba)-evoked currents at its higher concentrations [1]. | [in vivo]
animal models of epileptic seizures showed that retigabine treatment was effective at an oral dose as low as 0.01 mg/kg. studies performed in mice also indicated that combining retigabine with another anticonvulsant agent leads to an additive effect [1]. | [References]
[1] ferron gm,patat a,parks v,rolan p,troy sm. lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects. br j clin pharmacol.2003 jul;56(1):39-45. |
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