1404188-93-7
Chemical Structure
TAT-GluA2 3Y
- CAS No.: 1404188-93-7
- Formula:C115H185N43O29
- Molecular Weight:2633.97
IUPAC Name: (5S,8S,11S,14S,20S)-20-((2S,5S,8S,11S,14S,17S,20S,23S,26S,29S,32S,38S)-38-amino-17-(3-amino-3-oxopropyl)-2,26,29-tris(4-aminobutyl)-8,11,14,20,23,32-hexakis(3-guanidinopropyl)-5-(4-hydroxybenzyl)-39-(4-hydroxyphenyl)-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxo-3,6,9,12,15,18,21,24,27,30,33,36-dodecaazanonatriacontanamido)-11-(2-amino-2-oxoethyl)-5,14-bis(4-hydroxybenzyl)-8-isopropyl-4,7,10,13,16,19-hexaoxo-3,6,9,12,15,18-hexaazatricosanedioic acid
InChIKey: JRFBJZYZNDUYJM-NOEVYFGRSA-N
SMILES: OC(C=C1)=CC=C1C[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CCC(O)=O)C(NCC(N[C@H](C(N[C@@H](CC(N)=O)C(N[C@@H](C(C)C)C(N[C@H](C(NCC(O)=O)=O)CC2=CC=C(C=C2)O)=O)=O)=O)CC3=CC=C(C=C3)O)=O)=O)=O)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCC(N)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCCN)NC([C@H](CCCCN)NC([C@H](CCCNC(N)=N)NC(CNC([C@@H](N)CC4=CC=C(C=C4)O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction[1][2][3][4][5].
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TAT-GluA2 3Y | 99.93% | TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction. | ||||||||||||||||||||
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- [1]. Li W, et al. AMPA receptor potentiation alleviates NLRP3 knockout-induced fear generalization in mice. Biochem Biophys Res Commun. 2024;722:150074. [Content Brief]
- [2]. Lu H, et al. Synaptotagmin-3 interactions with GluA2 mediate brain damage and impair functional recovery in stroke. Cell Rep. 2023;42(3):112233. [Content Brief]
- [3]. Chen Z, et al. Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulation of GluA2 and GluA1 subunits by p38 MAPK and JNK. J Neurosci. 2014;34(29):9621-9643. [Content Brief]
- [4]. Choi FY, et al.Interference with AMPA receptor endocytosis: effects on behavioural and neurochemical correlates of amphetamine sensitization in male rats. J Psychiatry Neurosci. 2014 May;39(3):189-99. [Content Brief]
- [5]. Dias C, et al. Facilitated extinction of morphine conditioned place preference with Tat-GluA2(3Y) interference peptide. Behav Brain Res. 2012 Aug 1;233(2):389-97. [Content Brief]
Keywords
