Conantokin G

Names

[ Name ]:
Conantokin G

[Synonym ]:
'SLEEPER PEPTIDE'
H-GLY-GLU-GLA-GLA-LEU-GLN-GLA-ASN-GLN-GLA-LEU-ILE-ARG-GLA-LYS-SER-ASN-NH2
conotoxin GV
M.W. 2264.1 C88H138N26O44
GLY-GLU-GLA-GLA-LEU-GLN-GLA-ASN-GLN-GLA-LEU-ILE-ARG-GLA-LYS-SER-ASN-NH2
Conotoxin GV,Sleeper Peptide

Biological Activity

[Description]:

Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[References]

[1]. S D Donevan, et al. Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors. Mol Pharmacol. 2000 Sep;58(3):614-23.

[2]. A J Williams, et al. Neuroprotective efficacy and therapeutic window of the high-affinity N-methyl-D-aspartate antagonist conantokin-G: in vitro (primary cerebellar neurons) and in vivo (rat model of transient focal brain ischemia) studies. J Pharmacol Exp Ther. 2000 Jul;294(1):378-86.

Chemical & Physical Properties

[ Molecular Formula ]:
C₈₈H₁₃₈N₂₆O₄₄

[ Molecular Weight ]:
2264.19000

[ Exact Mass ]:
2262.94000

[ PSA ]:
1225.52000

[ Storage condition ]:
-20°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Articles

NMDA/NR2B selective antagonists in the treatment of ischemic brain injury.

Curr. Drug Targets. CNS Neurol. Disord. 4(2) , 143-51, (2005)

Glutamate is the main excitatory neurotransmitter in the central nervous system and it plays a significant role not only in synaptic transmission but also in acute and chronic neuropathologies includi...

The effect of CGX-1007 and CI-1041, novel NMDA receptor antagonists, on NMDA receptor-mediated EPSCs.

Epilepsy Res. 59(1) , 13-24, (2004)

The N-methyl-D-aspartate (NMDA) receptor-gated ion channel is comprised of at least one NR1 subunit and any of four NR2 subunits (NR2A-D). The NR2 subunit confers different pharmacological and kinetic...

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.

Neuropharmacology 57(2) , 127-36, (2009)

The conantokins are short, naturally occurring peptides that inhibit ion flow through N-methyl-d-aspartate receptor (NMDAR) channels. One member of this peptide family, conantokin-G (con-G), shows hig...