CGS 19755

CGS 19755 (Selfotel) is a highly selective, potent and competitive N-methyl-D-aspartate (NMDA) receptor antagonist. The compound binds directly to the postsynaptic NMDA receptor, competing with glutamate. CGS 19755 is a racemic mixture and a rigid analogue of 2-amino-5-phosphonopenranoic acid (AP5). The compound demonstrates anticonvulsant, anxiolytic and anti-ischemic effects. Clinically, intravenous administration of CGS 19755 is preferential over oral administration as the drug is not very active when administered orally^1,2. Several studies have found that CGS 19755 has the ability to limit neuronal damage in animal stroke models.

NMDA receptors play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. They mediate physiological functions such as learning and memory formation. These receptors play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions³. NMDA antagonists are effective in limiting ischemic damage to the brain and spinal cord. As shown in several studies, this compound has the ability to prevent ischaemia-induced hippocampal cell damage in gerbils.

These anti-ischemic properties make this compound an attractive application for clinical investigation^4,5.