product summary
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company name :
Alomone Labs
product type :
chemical
product name :
Retigabine
catalog :
R-100
more info or order :
citations: 32
Reference
Wu B, Su X, Zhang W, Zhang Y, Feng X, Ji Y, et al. Oxaliplatin Depolarizes the IB4- Dorsal Root Ganglion Neurons to Drive the Development of Neuropathic Pain Through TRPM8 in Mice. Front Mol Neurosci. 2021;14:690858 pubmed publisher
Villalba Galea C. Modulation of KV7 Channel Deactivation by PI(4,5)P2. Front Pharmacol. 2020;11:895 pubmed publisher
Laumet G, Edralin J, Dantzer R, Heijnen C, Kavelaars A. CD3+ T cells are critical for the resolution of comorbid inflammatory pain and depression-like behavior. Neurobiol Pain. 2020;7:100043 pubmed publisher
Larsson J, Karlsson U, Wu X, Liin S. Combining endocannabinoids with retigabine for enhanced M-channel effect and improved KV7 subtype selectivity. J Gen Physiol. 2020;152: pubmed publisher
Goff K, Goldberg E. Vasoactive intestinal peptide-expressing interneurons are impaired in a mouse model of Dravet syndrome. elife. 2019;8: pubmed publisher
Feng M, Crowley N, Patel A, Guo Y, Bugni S, Luscher B. Reversal of a Treatment-Resistant, Depression-Related Brain State with the Kv7 Channel Opener Retigabine. Neuroscience. 2019;406:109-125 pubmed publisher
Kang S, Li J, Zuo W, Chen P, Gregor D, Fu R, et al. Downregulation of M-channels in lateral habenula mediates hyperalgesia during alcohol withdrawal in rats. Sci Rep. 2019;9:2714 pubmed publisher
Laumet G, Edralin J, Dantzer R, Heijnen C, Kavelaars A. Cisplatin educates CD8+ T cells to prevent and resolve chemotherapy-induced peripheral neuropathy in mice. Pain. 2019;160:1459-1468 pubmed publisher
Megat S, Ray P, Moy J, Lou T, Barragán Iglesias P, Li Y, et al. Nociceptor Translational Profiling Reveals the Ragulator-Rag GTPase Complex as a Critical Generator of Neuropathic Pain. J Neurosci. 2019;39:393-411 pubmed publisher
Tirko N, Eyring K, Carcea I, Mitre M, Chao M, Froemke R, et al. Oxytocin Transforms Firing Mode of CA2 Hippocampal Neurons. Neuron. 2018;100:593-608.e3 pubmed publisher
Brueggemann L, Cribbs L, Schwartz J, Wang M, Kouta A, Byron K. Mechanisms of PKA-Dependent Potentiation of Kv7.5 Channel Activity in Human Airway Smooth Muscle Cells. Int J Mol Sci. 2018;19: pubmed publisher
Paz R, Tubert C, Stahl A, Díaz A, Etchenique R, Murer M, et al. Inhibition of striatal cholinergic interneuron activity by the Kv7 opener retigabine and the nonsteroidal anti-inflammatory drug diclofenac. Neuropharmacology. 2018;137:309-321 pubmed publisher
Ghezzi F, Monni L, Nistri A. Functional up-regulation of the M-current by retigabine contrasts hyperexcitability and excitotoxicity on rat hypoglossal motoneurons. J Physiol. 2018;596:2611-2629 pubmed publisher
Hu W, Bean B. Differential Control of Axonal and Somatic Resting Potential by Voltage-Dependent Conductances in Cortical Layer 5 Pyramidal Neurons. Neuron. 2018;97:1315-1326.e3 pubmed publisher
Vanhoof Villalba S, Gautier N, Mishra V, Glasscock E. Pharmacogenetics of KCNQ channel activation in 2 potassium channelopathy mouse models of epilepsy. Epilepsia. 2018;59:358-368 pubmed publisher
Lee C, Holt J, Jones T. Effect of M-current modulation on mammalian vestibular responses to transient head motion. J Neurophysiol. 2017;118:2991-3006 pubmed publisher
Laumet G, Zhou W, Dantzer R, Edralin J, Huo X, Budac D, et al. Upregulation of neuronal kynurenine 3-monooxygenase mediates depression-like behavior in a mouse model of neuropathic pain. Brain Behav Immun. 2017;66:94-102 pubmed publisher
Rubi L, Kovar M, Zebedin Brandl E, Koenig X, Dominguez Rodriguez M, Todt H, et al. Modulation of the heart's electrical properties by the anticonvulsant drug retigabine. Toxicol Appl Pharmacol. 2017;329:309-317 pubmed publisher
Greene D, Kang S, Hoshi N. XE991 and Linopirdine Are State-Dependent Inhibitors for Kv7/KCNQ Channels that Favor Activated Single Subunits. J Pharmacol Exp Ther. 2017;362:177-185 pubmed publisher
Kang S, Li J, Zuo W, Fu R, Gregor D, Krnjevic K, et al. Ethanol Withdrawal Drives Anxiety-Related Behaviors by Reducing M-type Potassium Channel Activity in the Lateral Habenula. Neuropsychopharmacology. 2017;42:1813-1824 pubmed publisher
Krukowski K, Ma J, Golonzhka O, Laumet G, Gutti T, Van Duzer J, et al. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017;158:1126-1137 pubmed publisher
Nassoiy S, Byron K, Majetschak M. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements after hemorrhagic shock in rats. J Biomed Sci. 2017;24:8 pubmed publisher
Ghezzi F, Corsini S, Nistri A. Electrophysiological characterization of the M-current in rat hypoglossal motoneurons. Neuroscience. 2017;340:62-75 pubmed publisher
Rinker J, Fulmer D, Trantham Davidson H, Smith M, Williams R, Lopez M, et al. Differential potassium channel gene regulation in BXD mice reveals novel targets for pharmacogenetic therapies to reduce heavy alcohol drinking. Alcohol. 2017;58:33-45 pubmed publisher
Kim K, Duignan K, Hawryluk J, Soh H, Tzingounis A. The Voltage Activation of Cortical KCNQ Channels Depends on Global PIP2 Levels. Biophys J. 2016;110:1089-98 pubmed publisher
Corbin Leftwich A, Mossadeq S, Ha J, Ruchala I, Le A, Villalba Galea C. Retigabine holds KV7 channels open and stabilizes the resting potential. J Gen Physiol. 2016;147:229-41 pubmed publisher
Liu C, Glowatzki E, Fuchs P. Unmyelinated type II afferent neurons report cochlear damage. Proc Natl Acad Sci U S A. 2015;112:14723-7 pubmed publisher
Sobieski C, Jiang X, Crawford D, Mennerick S. Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro. J Neurosci. 2015;35:11105-17 pubmed publisher
Sheppard A, Chen G, Salvi R. Potassium ion channel openers, Maxipost and Retigabine, protect against peripheral salicylate ototoxicity in rats. Hear Res. 2015;327:1-8 pubmed publisher
Svalø J, Sheykhzade M, Nordling J, Matras C, Bouchelouche P. Functional and molecular evidence for Kv7 channel subtypes in human detrusor from patients with and without bladder outflow obstruction. PLoS ONE. 2015;10:e0117350 pubmed publisher
Qi Y, Wang J, Bomben V, Li D, Chen S, Sun H, et al. Hyper-SUMOylation of the Kv7 potassium channel diminishes the M-current leading to seizures and sudden death. Neuron. 2014;83:1159-71 pubmed publisher
Vetter I, Hein A, Sattler S, Hessler S, Touska F, Bressan E, et al. Amplified cold transduction in native nociceptors by M-channel inhibition. J Neurosci. 2013;33:16627-41 pubmed publisher
image
image 1 :
Alomone Labs R-100 image 1
Alomone LabsTelmisartaninhibits the activation of AT1R expressed in CHO-K1-mt aequorin-G?16 cells. - Dose response curve for the inhibition of AT1R expressed in CHO-K1-mt aequorin-G?16 cells. Ca2+response as detected by elevation in aequorin derived fluorescence following 0.04 nM Angiotensin II application was inhibited by increasing concentrations ofTelmisartan(T-170). 500 nM Telmisartan fully inhibited the activation by Angiotensin II.
product information
CAT :
R-100
SKU :
R-100_10 mg
Product Name :
Retigabine
Group Type :
Non Antibodies
Product Type :
S. Molecules
Storage After Reconstitution :
The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.
Shipping and storage :
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Product Page - Scientific background :
The KCNQ family of voltage-gated K+ channels includes five known members: KCNQ1 to KCNQ5. Structurally, the KCNQ family belongs to the six transmembrane domain category of K+ channels. KCNQ family members can form either homomultimeric or heteromultimeric channels with different functional consequences. For example, KCNQ2 and KCNQ3 heteromultimers give rise to a much larger channel current than when either protein is expressed alone. Indeed, KCNQ2/KCNQ3 heteromultimers are believed to be the molecular correlates of the so-called M current. This current is a K+ neuronal current that is strongly inhibited by the activation of the M1 subtype of the muscarinic acetylcholine receptor. Mutations in either KCNQ2 or KCNQ3 are associated with a form of epilepsy known as benign familial neonatal convulsions (BNFC)1-3.Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)4-7, which is used in the clinic to treat epilepsy8. Retigabine (0.1 to 10 µM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells5 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.46. Similar effects were seen with 10 µM retigabine in oocytes expressing the KV7.2/3 heteromeric channel7.
Supplier :
Alomone Labs
Target :
KCNQ2, KCNQ3, and KCNQ4 K+ channels
Long Description :
Retigabine (#R-100) is a highly pure, synthetic, and biologically active compound.
Short Description :
A Potent and Selective Modulator of KCNQ Channels
MW :
303.3
Synonyms :
D-23129, Ezogabine, Trobalt®, Potiga®
Source :
Synthetic
Molecular formula :
C16H18FN3O2.
Effective Concentration :
0.1-100 µM.
Activity :
Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1-4, which is used in the clinic to treat epilepsy5. Retigabine (0.1 to 10 μM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells2 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.43. Similar effects were seen with 10 μM retigabine in oocytes expressing the KV7.2/3 heteromeric channel4.
Reconstitution and Solubility :
Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Solubility :
DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions :
Up to four weeks at 4°C or three months at -20°C.
Lead Time :
1-2 Business Days
Country of origin :
Israel/IL
Applications key :
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Purity :
>99% (HPLC)
CAS No :
150812-12-7
Form :
Lyophilized Powder
Comment :
Contact Alomone Labs for technical support and product customization
UNSPSC :
41116134
Bioassay Tested :
Yes
Cited Application :
Electrophysiology
Chemical Name :
Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate.
more info or order :
company information
Alomone Labs
Jerusalem BioPark (JBP), Hadassah Ein Kerem
P.O. Box 4287
Jerusalem 9104201
info@alomone.com
http://www.alomone.com
972 2 531 8002
headquarters: Israel