Overview
- Fagg, G.E. et al. (1990) Br. J. Pharmacol. 99, 791.
Alomone Labs CGP-37849 inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 50 µM glutamate + 50 µM glycine every 50 sec, while membrane potential was held at -60 mV. 4 min applications of 5 nM and 25 nM CGP-37849 (#C-325) reversibly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control, 5 nM and 25 nM CGP-37849 (as indicated).
CGP-37849 is a synthetic compound that acts as a potent, selective, and competitive antagonist of N-methyl-d-aspartate (NMDA) receptors. CGP 37849 shows significant central effects following oral administration to animals. CGP-37849 is used to elucidate the roles of NMDA receptors in brain function, and as therapeutic agents for the treatment of neurological disorders such as epilepsy and ischemic brain damage in humans1.
NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play important roles in a variety of cellular processes and brain functions such as synaptic plasticity, addiction, and stroke. NMDA receptors mediate physiological functions such as learning and memory formation and participate in glutamate excitotoxicity2.
