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Riluzole hydrochloride
Chemical Name:2-Amino-6-trifluoromethoxybenzothiazole hydrochloride
Biological Activity:
Novel psychotropic agent with
anticonvulsant, hypnotic, anxiolytic, anti-ischaemic and anaesthetic
properties. Riluzole is able to act as a glutamate release inhibitor, blocks
voltage-dependent Na+ channels and inhibits GABA uptake by striatal
synaptosomes.
Benazzouz et al (1995) Riluzole prevents MPTP-induced parkinsonism in the
rhesus monkey: a pilot study. Eur.J.Pharmacol. 284 299. Umeniya
and Berger (1995) Inhibition by riluzole of glycinergic postsynaptic
currents in rat hypoglossal motoneurones. Br.J.Pharmacol. 116 3227.
Taylor and Meldrum (1995) Na+ channels as targets for
neuroprotective drugs. TiPS. 16 309. Songet al
(1997) Differential action of riluzole on tetrodotoxin-sensitive and
tetrodotoxin-resistant sodium channels. J.Pharmacol.Exp.Ther. 282
707.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.