Conantokin G
Conantokin G structure
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Common Name | Conantokin G | ||
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| CAS Number | 93438-65-4 | Molecular Weight | 2264.19000 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C88H138N26O44 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
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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 including stroke. Presently, four receptors for glutamate have bee... |
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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 properties to the receptor. CGX-1007 (Conantokin G), a 17-... |
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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 high selectivity for antagonism of NR2B-containing NMDAR chann... |
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Conantokins inhibit NMDAR-dependent calcium influx in developing rat hippocampal neurons in primary culture with resulting effects on CREB phosphorylation.
Mol. Cell. Neurosci. 45(2) , 163-72, (2010) The effects of conantokin (con)-G, con-R[1-17], and con-T on ion flow through N-methyl-D-aspartate receptor (NMDAR) ion channels were determined in cultured primary rat hippocampal neurons. The potency of con-G diminished, whereas inhibition by con-R[1-17] an... |
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Blockade of hindbrain NMDA receptors containing NR2 subunits increases sucrose intake.
Am. J. Physiol. Regul. Integr. Comp. Physiol. 296(4) , R921-8, (2009) We have previously shown that blockade of N-methyl-d-aspartate (NMDA) receptors in the caudal brain stem delays satiation and increases food intake. NMDA receptors are heterodimers made up of distinct, but different, ion channel subunits. The NR2 subunits of ... |
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CGX-1007 prevents excitotoxic cell deathviaactions at multiple types of NMDA receptors
Neurotoxicology 32 , 392-399, (2011) Glutamate induced excitotoxic injury through over-activation of N-methyl-D-aspartate receptors (NMDARs) plays a critical role in the development of many neurodegenerative diseases. The present study was undertaken to evaluate the role of CGX-1007 (Conantokin ... |
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NR2B-selective conantokin peptide inhibitors of the NMDA receptor display enhanced antinociceptive properties compared to non-selective conantokins.
Neuropeptides 42(5-6) , 601-9, (2008) NR2B-selective inhibitors show lower side-effects in preclinical pain models than non-selective NMDA receptor (NMDAR) antagonists, but it is unclear whether the improved safety of NR2B-selective inhibitors is due to their subtype selectivity or to a unique mo... |
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Effect of Conantokin G on NMDA receptor-mediated spontaneous EPSCs in cultured cortical neurons.
J. Neurophysiol. 96(3) , 1084-92, (2006) Conantokin G (Con G), derived from the venom of Conus geographus, is the most characterized natural peptide antagonist targeted to N-methyl-D-aspartate (NMDA) receptors. Although Con G is known to bind to the glutamate binding site on the NR2 subunit of the r... |
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A single amino acid replacement results in the Ca2+-induced self-assembly of a helical conantokin-based peptide.
Biochemistry 43(41) , 13225-32, (2004) Conantokins are short (17-27 amino acid residues), gamma-carboxyglutamate (Gla)-rich peptide components of the venoms of marine snails of the genus Conus. They display high apo and/or Ca(2+)-induced helicity and act as potent and selective inhibitors of the N... |
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Specific determinants of conantokins that dictate their selectivity for the NR2B subunit of N-methyl-D-aspartate receptors.
Neuroscience 170 , 703-710, (2010) Conantokins are naturally-occurring small peptide antagonists of ion flow through NMDA/glycine activated-N-methyl-d-aspartate receptor (NMDAR) ion channels. One member of the conantokin family, conantokin (con)-G, a 17-residue peptide, is selective for NMDARs... |