Tri- and tetra-substituted guanidines and their use as excitator

Details Tri- and tetra-substituted guanidines and their use as excitator Tri- and tetra-substituted guanidines and their use as excitator

1995-05-22

1998-08-25

O'Sullivan, Peter

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514183, 514457, 549288, 552 8, 564230, 564237, 564238, 564239, 564240, A61K 31155, A61K 31655, A61K 3137, C07C27918

Patent

active

057983909

ABSTRACT:
Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of 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 neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

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