1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Potassium Channel
    iGluR

Flupirtine Maleate 

Cat. No.: HY-17001 Purity: 99.97%
Handling Instructions

Flupirtine Maleate(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.

For research use only. We do not sell to patients.

Flupirtine Maleate Chemical Structure

Flupirtine Maleate Chemical Structure

CAS No. : 75507-68-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
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Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
500 mg USD 391 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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Other Forms of Flupirtine Maleate:

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  • Technical Information

  • Purity & Documentation

  • References

Description

Flupirtine Maleate(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. IC50 Value: Target: Potassium channel; NMDA receptor in vitro: High concentrations of flupirtine antagonized inward currents to NMDA(200 microM) at -70 mV with an lC50 against steady-state responses of 182.1+/-12.1 microM. The effects of flupirtine were voltage-independent and not associated with receptor desensitization making actions within the NMDA receptor channel or at the glycine modulatory site unlikely. NMDA receptor antagonism probably has little relevance for the clinical efficacy of flupirtine as the concentrations needed were far higher than those achieved in clinical practice. However, the activation of a G-protein-regulated inwardly rectifying K+ channel was identified as an interesting molecular target site of flupirtine. In the next stage, the central nervous spectrum of action of experimental K+ channel openers (PCO) was considered. As far as they have been studied, experimental K+ channel openers display a spectrum of action comparable to that of flupirtine [1]. Therapeutic flupirtine concentrations (≤10 μM) did not affect voltage-gated Na(+) or Ca(2+) channels, inward rectifier K(+) channels, nicotinic acetylcholine receptors, glycine or ionotropic glutamate receptors. Flupirtine shifted the gating of K(V)7 K(+) channels to more negative potentials and the gating of GABA(A) receptors to lower GABA concentrations [2]. Cell exposure to flupirtine decreased the amplitude of delayed rectifier K(+) current (I(K(DR))) with a concomitant raise in current inactivation in NSC-34 neuronal cells [4]. in vivo: Rats were trained to discriminate the novel analgesic flupirtine (10.0 mg/kg i.p., 10 min) from no drug under a two-choice fixed-ratio 5 shock-termination schedule. Flupirtine yielded a dose-response curve with an ED50 of 3.87 mg/kg. The opioid analgesics pentazocine, codeine and tramadol failed to produce flupirtine appropriate responding. The opioid antagonist naltrexone did not antagonize the discriminative effects of flupirtine [3]. Both morphine (ED50=0.74 mg/kg) and flupirtine (ED50=3.32 mg/kg) caused dose-related anti-hyperalgesia at doses that did not cause sedation [5]. Toxicity: Based on study-end data, hepatotoxicity was detected in 31% of patients receiving flupirtine for ≥ 6 weeks [6].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (95.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3787 mL 11.8937 mL 23.7874 mL
5 mM 0.4757 mL 2.3787 mL 4.7575 mL
10 mM 0.2379 mL 1.1894 mL 2.3787 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

420.39

Formula

C₁₉H₂₁FN₄O₆

CAS No.

75507-68-5

SMILES

O=C(NC1=CC=C(N=C1N)NCC2=CC=C(C=C2)F)OCC.O=C(/C=C\C(O)=O)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.97%

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Product Name:
Flupirtine Maleate
Cat. No.:
HY-17001
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Flupirtine Maleate

Cat. No.: HY-17001