Abstract: Disclosed is a method for identifying compounds that bind to or modulate a glutamate transporter. The disclosed method is useful for identifying compounds that can inhibit, stimulate, or modulate the activity of the glutamate transporter and thus affect glutamate reuptake. The method is a screening technique where compounds known to bind to glutamate receptors (for example, glutamate receptor ligands, including many agonists, and antagonists) are bound to a glutamate transporter and compounds are screened to identify those that can alter the binding of the glutamate receptor-binding compounds. Compounds shown to alter the binding of the receptor compounds from glutamate transporters in the disclosed assay can have a variety of effects on glutamate transporter activity including activation or inhibition. These compounds are expected to affect or interfere with glutamate reuptake by the glutamate transporter and thus can be used to modulate, stimulate, or inhibit glutamate reuptake.

Abstract: A class of heterocyclic amino-alcohol compounds is described for treatment of CNS-related diseases, namely, for use as a neuroprotective agent, to reduce neurotoxic injury associated with conditions of hypoxia, anoxia or ischemia which typically follows stroke, myocardial infarct, perinatal asphyxia, or hypoglycemic events. Other examples of treatable CNS-related diseases include neurodegenerative diseases such as Parkinson's disease, Huntington's chorea and Alzheimer's disease, and also psychotic disorders such as schizophrenia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as a mediator to alter excitatory actions at the NMDA excitatory amino acid receptor complex.