conantokin R

Potent, non-competitive NMDA receptor antagonist (IC50= 93 nM) that has been suggested to have NR2 subunit selectivity. Inhibits inward currents evoked by NMDA in central nervous system neurons (IC50= 350 nM) and exhibits broad anticonvulsant and antiparkinsonian activityin vivoat doses devoid of behavioral toxicity.

Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC50 of 93 nM. Conantokin R binds Zn2+ and Mg2+ with Kds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity[1][2].

[1] Blandl T, et al. Structure-function relationships of the NMDA receptor antagonist peptide, conantokin-R. FEBS Lett. 2000 Mar 24;470(2):139-46. DOI:10.1016/s0014-5793(00)01309-0
[2] White HS, et al. In vitro and in vivo characterization of conantokin-R, a selective NMDA receptor antagonist isolated from the venom of the fish-hunting snail Conus radiatus. J Pharmacol Exp Ther. 2000 Jan;292(1):425-32. PMID:10604979