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Selective inhibitor of NR2B-containing NMDAR

Conantokin-G is a conopeptide that has been isolated from the venom of the cone Conus geographus. Conantokin-G selectively inhibits NR2B containing N-methyl-D-aspartate receptors (NMDAR) with a high specificity. Thus, Conantokin-G inhibits in a concentration-dependent manner the Ca2+ influx leading to a neuroprotective effect against NMDA-induced excitotoxicity. Conantokin-G was shown to block NMDA-evoked currents in murine cortical neurons with an IC50 value of around 480 nM.

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AA sequence: Gly-Glu-Gla-Gla-Leu-Gln-Gla-Asn-Gln-Gla-Leu-Ile-Arg-Gla-Lys-Ser-Asn-NH2
Length (aa): 17
Formula: C88H138N26O44
Molecular Weight: 2264.23 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: [93438-65-4] Source: Synthetic
Purity rate: > 95 %

Opposing action of conantokin-G on synaptically and extrasynaptically-activated NMDA receptors

CGX-1007 prevents excitotoxic cell death via actions at multiple types of NMDA receptors

Specific determinants of conantokins that dictate their selectivity for the NR2B subunit of N-methyl-D-aspartate receptors.

The selectivity of conantokin-G for ion channel inhibition of NR2B subunit-containing NMDA receptors is regulated by amino acid residues in the S2 region of NR2B

Powerful antinociceptive effects of the cone snail venom-derived subtype-selective NMDA receptor antagonists conantokins G and T

The amino acid residue at sequence position 5 in the conantokin peptides partially governs subunit-selective antagonism of recombinant N-methyl-D-aspartate receptors

Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors.

Binding of cations to individual gamma-carboxyglutamate residues of conantokin-G and conantokin-T

NMDA-receptor antagonist requirements in conantokin-G.

Conantokin-G: a novel peptide antagonist to the N-methyl-D-aspartic acid (NMDA) receptor

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