Drug intelligence / Profile preview

conantokin-G

Development stage
Preclinical
Lead developer
Cognetix
Modality
Peptides
Administration
Intracerebroventricular, Intrathecal, Not Generally Systemic/oral
01

Overview

**Conantokin-G** is a 17-amino-acid peptide toxin originally isolated from the venom of the marine cone snail *Conus geographus*. It is a highly selective and potent antagonist of the N-methyl-D-aspartate (NMDA) receptor, specifically targeting receptors containing the GluN2B (also known as NR2B) subunit. Unlike many other NMDA antagonists, conantokin-G demonstrates subunit specificity, which may result in a more favorable in vivo pharmacological profile. Mode of action is primarily competitive at the glutamate-binding site of the NR2B subunit, leading to inhibition of NMDA-evoked calcium influx, neuroexcitotoxicity, and associated neuronal death. Preclinical evidence demonstrates anti-apoptotic, anti-convulsant, anti-analgesic, and neuroprotective effects, including robust protection in models of ischemic brain injury. As a peptide containing γ-carboxyglutamate residues, it is structurally distinct from traditional small molecule NMDA antagonists[1][2][3][4][5][6][7][9][12].

Other names
conantokin GCon-GCGX-1007CGX1007CGX 1007
02

Targets

GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)

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