Non-competitive inhibitor of NMDA glutamatergic receptors acting at the polyamine site. Conantokin G (CGX-1007), a member of the conantokin family, is a selective NR2B subunit inhibitor of NMDA glutamatergic receptors with activity as a neuroprotective agent against NMDA-induced excitotoxicity.
The most selective and potent non-competitive antagonist among the members of the conantokin peptide family for NR2B-containing NMDAR channels (Ki = 0.8 μM with close to 100% inhibition of NR1/NR2B mediated current). Widely used for studies related to NMDAR neurotransmissions in both peripheral and center nervous systems.
Primary TargetNMDA receptors