Flupirtine maleate

Description

Flupirtine maleate is a centrally-acting, non-addicting analgesic agent somewhat more potent than aspirin, paracetamol and pentazocine. It is reported to be useful in the treatment of postoperative and dental pain.

Description

Flupirtine is an activator of voltage-gated potassium channel 7 (K_v7/KCNQ). It induces relaxation of preconstricted pulmonary arteries isolated from wild-type and serotonin transporter-overexpressing (SERT⁺) mice. Flupirtine (30 mg/kg per day) decreases mean right ventricular pressure and right ventricular hypertrophy in hypoxia-induced and SERT⁺ mouse models of pulmonary arterial hypertension. It increases the paw withdrawal threshold in a rat model of streptozotocin-induced diabetic neuropathy when administered at a dose of 10 mg/kg and increases paw withdrawal latency in a rat model of carrageenan-induced paw inflammation when used in combination with morphine. Flupirtine also indirectly antagonizes NMDA receptors via its effects on potassium channels.

Chemical properties

Off-White Solid

Originator

Chemiewerk Homburg (Degussa) (W. Germany)

The Uses of Flupirtine maleate

Analgesic. Substituted pyridine with central analgesic properties.

The Uses of Flupirtine maleate

Analgesic. Substituted pyridine with central analgesic properties. A potassium channel opener.

What are the applications of Application

Flupirtine Maleate is an indirect NMDA antagonist and Potassium channel activator

brand name

KATADOLAN

Biological Activity

Non-opioid analgesic with muscle relaxant properties. Activates K + channels and indirectly antagonizes NMDA receptors. Exhibits neuroprotective actions in a model of cerebral ischemia in mice and reduces apoptosis and necrosis induced by noxious stimuli.

storage

Desiccate at +4°C

References

1) Azad?et al. (2004), The potassium channel modulator flupirtine shifts the frequency-response function of hippocampal synapses to favour LTD in mice; Neuro. Sci. Lett.,?370?186 2) Klinger?et al.?(2012),?Concomitant facilitation of GABAA receptors and KV7 channels by the non-opioid analgesic flupirtine; Br. J. Pharmacol.,?166?1631 3) Osbourne?et al. (1998),?Flupirtine, a nonopioid centrally acting analgesic, acts as an NMDA antagonist; Gen. Pharmacol.,?30?255