Retigabine

Catalog No.S4733 Synonyms: N-(2-amino-4-[fluorobenzylamino]-phenyl) carbamic acid|D-23129

Retigabine Chemical Structure

Molecular Weight(MW): 303.33

Retigabine(free base) 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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Biological Activity

Description Retigabine(free base) 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]
()
KCNQ2/Q3 channels [2]
()
KCQN4 [2]
()
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 differed 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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells NI\qUZJHfW6ldHnvckBie3OjeR?= NVL5dYJ{SWO2aY\peJkh[XRiS4[gO{4zKGOqYX7u[Ywh\XiycnXzd4VlKGmwIHPsc45m\CCFSF:gZ4VtdHNiYomgX|g3WmKfIHXm[ox2gCCjc4PhfUwhTUN3ME2wMlE2KM7:TR?= MlHkNVc1QDl3N{S=
HEK 293 cells MlnwSpVv[3Srb36gZZN{[Xl? NX\EN45vX2ixbHWtZ4VtdCCyYYTjbE1kdGGvcDDvckBz\WOxbXLpcoFvfCCvb4Xz[UBMS06TMjDjbIFvdmWuczDlfJBz\XO|ZXSgbY4hUEWNIEK5N{Bk\WyuczDheEAuPDBibW[sJGVEPTB;MT6zJO69VQ>? NILIenEyPTB3ME[0OC=>
RAW264.7 cells M1jjR2Z2dmO2aX;uJIF{e2G7 M2TCXWlvcGmkaYTpc44hd2ZiUFfFNkBxem:mdXP0bY9vKGmwIFzQV{1qdmS3Y3XkJI1wfXOnIGLBW|I3PC55IHPlcIx{NCCLQ{WwQVAvODB5IN88US=> MXGyOVQ2OzhyMB?=

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • 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 was 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]

+ Expand
  • Animal Models: DBA/2 mice
  • Formulation: Dissolved initially in dimethylsulphoxide (DMSO) and then hydroxymethylcellulose with a final concentration of 20% DMSO
  • Dosages: 0.5-20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (197.8 mM)
Ethanol 35 mg/mL (115.38 mM)
Water Insoluble

* 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 303.33
Formula

C16H18FN3O2

CAS No. 150812-12-7
Storage powder
in solvent
Synonyms N-(2-amino-4-[fluorobenzylamino]-phenyl) carbamic acid|D-23129

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01823159 Completed Drug: retigabine|Drug: placebo Epilepsy University Hospital of Mont-Godinne|GlaxoSmithKline|Université Catholique de Louvain April 2013 Phase 3
NCT01938560 Completed Other: Survey Responses Epilepsy GlaxoSmithKline February 2013 --
NCT01691872 Withdrawn Drug: Retigabine Epilepsy Partial GlaxoSmithKline October 10 2012 Phase 1
NCT01668654 Terminated Drug: retigabine/ezogabine Epilepsy GlaxoSmithKline|Bausch Health Americas Inc. September 4 2012 Phase 3
NCT01494584 Terminated Drug: ezogabine/retigabine Epilepsy GlaxoSmithKline|Bausch Health Americas Inc. July 25 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID