Retigabine 2HCl

For research use only.

Catalog No.S4734 Synonyms: N-(2-amino-4-[fluorobenzylamino]-phenyl) carbamic acid (2HCl), D-23129 2HCl

Retigabine 2HCl Chemical Structure

CAS No. 150812-13-8

Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.

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Description Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.
Targets
KCNQ3/5 [2]
(Cell-based assay)
KCNQ2/Q3 channels [2]
(Cell-based assay)
KCQN4 [2]
(Cell-based assay)
1.4 μM(EC50) 1.6 μM(EC50) 5.2 μM(EC50)
In vitro

Retigabine is a novel antiepileptic drug whose mechanism of action involves potassium channel opening activity in neuronal cells. Retigabine can markedly enhance KCNQ2/Q3 currents. In addition, retigabine also enhances slow channel deactivation. Retigabine has been shown to increase the synthesis of GABA in rat hippocampal slices and to enhance GABA-induced chloride currents in cultured rat cortical neurons. Retigabine has been shown to induce membrane hyperpolarization in neurones in rat hippocampal-entorhinal cortex slices and to exert potassium channel opening activity in neuronal cells. Retigabine enhances a linopirdine-sensitive current in differentiated PC12 cells[1]. concentrations of RTG/EZG ≥10 μM are required to cause significant augmentation of the GABAA receptor response. The potency of RTG/EZG differs somewhat depending on the GABAA receptor subunit combination, with the following rank order: α1β3γ2=α1β2γ2 >α3β2γ2=α2β2γ2>α5β2γ2=α1β2(N265S)γ2=α1β1γ2. RTG/EZG exhibits only weak inhibitory effects at voltage-gated Nav and Cav channel currents at predominantly supratherapeutic concentrations. RTG/EZG does not interact significantly with glutamate receptors[2].

In vivo Retigabine enhances γ-aminobutyric acid (GABA)-ergic transmission in the central nervous system[1]. Retigabine is rapidly absorbed and distributed with an oral bioavailability of 60% and a high volume of distribution of approximately 6.2 L/kg. Tolerability is good in humans when titrated up to its therapeutic dose range (600-1200 mg/day). Plasma protein binding of the drug is approximately 80%. The relatively high systemic bioavailability after oral administration suggests that retigabine is resistant to first-pass metabolism, a finding confirmed in multiple species. Retigabine is metabolized exclusively via phase II hepatic glucuronidation and acetylation. Gender differences in exposure have been noted, with female subjects exhibiting higher plasma concentrations of the drug after oral administration than male subjects. Excretion of retigabine appears to be predominantly renal. Depending on the behavioral endpoints analyzed, it appears that retigabine has a relatively poor therapeutic index (ratio between TD50 obtained in rotarod and ED50 obtained in maximal electroshock where maximal tonic extension of the hindlimbs was used as endpoint) in both mice (TD50/ED50 = 2.2) and rats (TD50/ED50 = 1.9) after i.p. administration. However, after p.o. administration in rats retigabine shows a therapeutic index of 28.8, which compares favorably with that reported for other antiepileptics, such as carbamazepine[4].

Protocol

Cell Research:

[3]

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  • Cell lines: HEK293 cells
  • Concentrations: 0.1, 0.3, 1 or 3 μM
  • Incubation Time: 4 h
  • Method:

    The retigabine incubation experiments are performed on HEK293 cells transfected with 10 ng KV2.1 over 48 h. 24 h post-transfection, HEK293 cells are either exposed to normal medium (control) containing 0.1% DMSO (vehicle control) or 0.1, 0.3, 1 or 3 μM retigabine for 4 h. After the 4 h exposure, the incubation medium is removed and fresh medium is added to the transfected HEK293 cells. Thus, at the moment of electrophysiological analysis (48 h post-transfection), no retigabine is present in the recording solution.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: DBA/2 mice
  • Dosages: 0.5-20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (199.33 mM)
Water 75 mg/mL (199.33 mM)
Ethanol 25 mg/mL (66.44 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 376.25
Formula

C16H18FN3O2.2HCl

CAS No. 150812-13-8
Storage powder
in solvent
Synonyms N-(2-amino-4-[fluorobenzylamino]-phenyl) carbamic acid (2HCl), D-23129 2HCl
Smiles CCOC(=O)NC1=C(C=C(C=C1)NCC2=CC=C(C=C2)F)N.Cl.Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID