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Retigabine

別名：D-23129, N-(2-amino-4-[fluorobenzylamino]-phenyl) carbamic acid

Retigabine (D-23129) 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.

Retigabine化学構造

CAS No. 150812-12-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 59500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Retigabine関連製品

シグナル伝達経路

Potassium Channel Signaling Pathways

Potassium Channelシグナル伝達経路

Potassium Channel阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
CHO cells Function assay Activity at Kv 7.2 channel expressed in cloned CHO cells by [86Rb] efflux assay, EC50=0.15 μM 17489574
HEK 293 cells Function assay Whole-cell patch-clamp on recombinant mouse KCNQ2 channels expressed in HEK 293 cells at -40 mV, EC50=1.3 μM 15050644
RAW264.7 cells Function assay Inhibition of PGE2 production in LPS-induced mouse RAW264.7 cells, IC50=0.007 μM 25453800
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生物活性

製品説明 Retigabine (D-23129) 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
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].
細胞実験 細胞株 HEK293 cells
濃度 0.1, 0.3, 1 or 3 μM
反応時間 4 h
実験の流れ

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.
In Vivo
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].
動物実験 動物モデル DBA/2 mice
投与量 0.5-20 mg/kg
投与経路 i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01823159 Completed
Epilepsy
University Hospital of Mont-Godinne|GlaxoSmithKline|Université Catholique de Louvain
 April 2013 Phase 3
NCT01938560 Completed
Epilepsy
GlaxoSmithKline
 February 2013 --
NCT01691872 Withdrawn
Epilepsy Partial
GlaxoSmithKline
 October 10 2012 Phase 1
NCT01668654 Terminated
Epilepsy
GlaxoSmithKline|Bausch Health Americas Inc.
 September 4 2012 Phase 3
NCT01494584 Terminated
Epilepsy
GlaxoSmithKline|Bausch Health Americas Inc.
 July 25 2012 Phase 2

化学情報

分子量 303.33 化学式

C16H18FN3O2
CAS No. 150812-12-7 SDF Download Retigabine SDFをダウンロードする
Smiles CCOC(=O)NC1=C(C=C(C=C1)NCC2=CC=C(C=C2)F)N
保管

In vitro
Batch:

DMSO : 60 mg/mL ( (197.8 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 35 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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