75507-68-5

溶解度:Soluble to 100 mM in DMSO and to 10 mM in ethanol

储存条件:Desiccate at +4°C

生物活性

A centrally acting, nonopioid analgesic; flupirtine has a functional profile similar to NMDA-receptor antagonists, but devoid of the typical side effects of these drugs; flupirtine exerts potent cyto- and neuroprotective actions in different in vivo and in vitro models.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.

参考文献

Osborne et al (1998) Flupirtine, a nonopioid centrally acting analgesic, acts as an NMDA antagonist. Gen.Pharmacol. 30 255. Azad et al (2004) The potassium channel modulator flupirtine shifts the frequency-response function of hippocampal synapses to favour LTD in mice. Neurosci.Lett. 370 186. Yeung et al (2007) Molecular expression and pharmacological identification of a role for Kv7 channels in murine vascular reactivity. Br.J.Pharmacol. 151 758.