M. Deryck, PROTECTION OF NEUROLOGICAL FUNCTION IN STROKE MODELS AND NEUROPROTECTIVE PROPERTIES OF LUBELUZOLE, Cerebrovascular diseases, 7, 1997, pp. 18-30
Lubeluzole, the S-isomer of a novel difluorobenzothiazole, is a neurop
rotective compound aimed at the treatment of acute ischaemic stroke. I
n a photochemical stroke model in rats, in which a neurological test w
as designed that is also relevant to other stroke models, intravenous
posttreatment with lubeluzole stereoselectively rescues sensorimotor f
unction (time window of 6 h) and reduces infarct size. Posttreatment w
ith lubeluzole also reduces infarct size after middle cerebral artery
occlusion in rats, attenuates delayed neuronal death after global isch
aemia, and may also act on mechanisms of cerebral oedema. The compound
normalizes peri-infarct neuronal excitability and blocks the rise of
peri-infarct extracellular concentration of glutamate. Lubeluzole down
regulates the nitric oxide synthase (NOS) pathway leading to neurotoxi
city and neuronal death. NOS pathway modulation may contribute to the
neuroprotective properties of lubeluzole.