LKT Labs

Biochemicals for Life Science Research

Flupirtine Maleate

Product ID F4583
Cas No. 75507-68-5
Purity ≥98%
Product Unit SizeCostQuantityStock
10 mg $93.00 In stock
25 mg $193.80 In stock
100 mg $620.10 In stock
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Description

Flupirtine maleate is an agonist at voltage-gated KCNQ/Kv7 K+ channels; opening of these channels on neurons facilitates M-current generation and decreases axonal excitability. In addition to its modulation of K+ channels, flupirtine maleate also inhibits NMDA receptors and shifts gating of GABA-A receptors to decrease circulating GABA concentrations. Flupirtine maleate is an effective non-sedative analgesic, showing benefit in clinical trials of neurosurgical patients. In animal models, this compound also attenuates development of and reverses established pulmonary arterial hypertension, suggesting antihypertensive activity.

Product Info

Cas No.

75507-68-5
Purity

≥98%
Formula

C15H17FN4O2 • C4H4O4
Formula Wt.

304.32
IUPAC Name

(Z)-but-2-enedioic acid;ethyl N-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate
Melting Point

174-175℃
Appearance

White to off white powder

Shipping and Storage

Store Temp

Ambient
Ship Temp

Ambient

Downloads

MSDS

F4583 MSDS PDF
Info Sheet

F4583 Info Sheet PDF

References

Yadav G, Choupoo S, Das SK, et al. Evaluating the Role of Flupirtine for Postcraniotomy Pain and Compare it With Diclofenac Sodium: A Prospective, Randomized, Double Blind, Placebo-controlled Study. J Neurosurg Anesthesiol. 2013 Jun 11. [Epub ahead of print]. PMID: 23764718.

Fleckenstein J, Sittl R, Averbeck B, et al. Activation of axonal Kv7 channels in human peripheral nerve by flupirtine but not placebo - therapeutic potential for peripheral neuropathies: results of a randomised controlled trial. J Transl Med. 2013 Feb 8;11:34. PMID: 23394517.

Klinger F, Geier P, Dorostkar MM, et al. Concomitant facilitation of GABAA receptors and KV7 channels by the non-opioid analgesic flupirtine. Br J Pharmacol. 2012 Jul;166(5):1631-42. PMID: 22188423.

Harish S, Bhuvana K, Bengalorkar GM, et al. Flupirtine: Clinical pharmacology. J Anaesthesiol Clin Pharmacol. 2012 Apr;28(2):172-7. PMID: 22557738.

Devulder J. Flupirtine in pain management: pharmacological properties and clinical use. CNS Drugs. 2010 Oct;24(10):867-81. PMID: 20839897.

Morecroft I, Murray A, Nilsen M, et al. Treatment with the Kv7 potassium channel activator flupirtine is beneficial in two independent mouse models of pulmonary hypertension. Br J Pharmacol. 2009 Aug;157(7):1241-9. PMID: 19508393.

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