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AssigneeState of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University
InventorsEckard Weber, John F. Keana
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Disubstituted guanidines, e.g., N,N'-di-m-tolyl guanidine, N,N'-di-o-ethylphenyl guanidine, N,N'-di-m-ethylphenyl guanidine, and N,N'-di-o-iodophenyl-guanidine, exhibit a high binding affinity to phenylcyclidine (PCP) receptors. These guanidine derivatives act as non-competitive blockers to glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeautic treatment of neuronal loss in ischemia, hypoxia, hypoglycemia, and brain and spinal cord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Huntington's disease, Down's Syndrome and other neurodegenerative disorders.
A neuroprotecting N,N'-disubstituted guanidine which exhibits a high binding activity with respect to the PCP receptor in mammalian nerve cells selected from the group consisting of N,N'-di-o-iodo-phenyl-guanidine;
A method for treating a disease of the nervous system in which the pathophysiology of the disorder involves excessive excitation of nerve cells by agonists of NMDA receptors comprising the administration to a mammal exhibiting symptoms of such disorders or susceptible to such disorders, a N,N'-disubstituted guanidine having a high affinity for the PCP receptor of the nerve cell in an amount effective to block the ion channel of the NMDA-receptor ion-channel complex.
A method of inhibiting NMDA receptor-ion channel related neurotoxicity comprising administering to a mammal a N,N'-disubstituted guanidine possessing a high affinity for the PCP receptor of a nerve cell, in an amount effective to inhibit the neurotoxicity.
Dependencies are inferred from the claim text.