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

Flupirtine(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 Chemical Structure

Flupirtine Chemical Structure

CAS No. : 56995-20-1

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Flupirtine

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Description

Flupirtine(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 M) 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 (ED = 0.74 mg/kg) and flupirtine (ED = 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].

IC50 & Target

NMDA Receptor

 

Clinical Trial
Molecular Weight

304.32

Formula

C15H17FN4O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (410.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2860 mL 16.4301 mL 32.8601 mL
5 mM 0.6572 mL 3.2860 mL 6.5720 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2860 mL 16.4301 mL 32.8601 mL 82.1504 mL
5 mM 0.6572 mL 3.2860 mL 6.5720 mL 16.4301 mL
10 mM 0.3286 mL 1.6430 mL 3.2860 mL 8.2150 mL
15 mM 0.2191 mL 1.0953 mL 2.1907 mL 5.4767 mL
20 mM 0.1643 mL 0.8215 mL 1.6430 mL 4.1075 mL
25 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2860 mL
30 mM 0.1095 mL 0.5477 mL 1.0953 mL 2.7383 mL
40 mM 0.0822 mL 0.4108 mL 0.8215 mL 2.0538 mL
50 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6430 mL
60 mM 0.0548 mL 0.2738 mL 0.5477 mL 1.3692 mL
80 mM 0.0411 mL 0.2054 mL 0.4108 mL 1.0269 mL
100 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8215 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Flupirtine
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HY-17001A
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