ConantokinG

ConantokinG用途

Conantokin G 是一种 17 个氨基酸的肽,是一种有效,选择性和竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。Conantokin G 抑制鼠皮质神经元中 NMDA 诱发的电流,IC50 为 480 nM,具有神经保护作用。

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ConantokinG名称

[ CAS 号 ]:
93438-65-4

[ 中文名 ]:
GLY-GLU-GLA-GLA-LEU-GLN-GLA-ASN-GLN-GLA-LEU-ILE-ARG-GLA-LYS-SER-ASN-NH2

[ 英文名 ]:
Conantokin G

[英文别名 ]:

'SLEEPER PEPTIDE'
conotoxin GV
M.W. 2264.1 C88H138N26O44
Conotoxin GV,Sleeper Peptide

ConantokinG生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[参考文献]

[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.

ConantokinG物理化学性质

[ 分子式 ]:
C₈₈H₁₃₈N₂₆O₄₄

[ 分子量 ]:
2264.19000

[ 精确质量 ]:
2262.94000

[ PSA ]:
1225.52000

[ 外观性状 ]:
白色冻干的固体

[ 储存条件 ]:
-20°C

ConantokinG安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

ConantokinG文献

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...

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