Therapeutic potential of PCP receptor ligands

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Abstract
Pharmacological control of excitatory pathways responding to the neu retransmitter L-glutamate in the central nervous system (CNS) is an exceedingly important goal, yet to be achieved in a clinically useful and safe fashion. One approach is the development of compounds that can modulate the excessive activation of N-methyl-D-aspartate (NMDA) receptors by glutamate during ischaemic events such as stroke. Certain compounds can effect this modulation, known as neuroprotection, by binding to the phencyclidine (PCP) receptor, which is located within an ion channel associated with the NMDA receptor. These ion channel blockers impede inward calcium ion flux and thus antagonise the agonist action of glutamate. This goal is particularly valuable as it relates to preventing the spread of neuronal degradation that is part of the pathological process associated with ischaemia, the result being improved neurological outcome of patients. At least three drugs are currently being evaluated in clinical trials for treatmen...