Overview
- Traynelis, S.F. et al. (2010) Pharmacol. Rev. 62, 405.
Alomone Labs CGS 19755 inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes.A. Time course of NMDA currents that were elicited by stimulation with 10 µM glutamate and 10 µM glycine every 50s, while membrane potential was held at -80 mV. 0.1, 1 and 10 µM CGS 19755 (#C-310), applied for 3 min as indicated, inhibited current amplitude. B. Superimposed current traces taken from experiment described in A.
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 orally1,2. 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 investigation4,5.
