Pep2-AVKI 

Pep2-AVKI is a selective peptide inhibitor of the binding of the AMPA receptor subunit (GluR2) at the C-terminal PDZ site to C-kinase (PICK1). Pep2-AVKI does not affect the binding of (AMPA-type glutamate receptor) GluA2 to GRIP or ABP. Pep2-AVKI does not increase the amplitude of AMPA currents. pep2-AVKI can be used to study neurological diseases^[1][2][3][4].

Pep2-AVKI (1 mM) selectively binds to PICK and does not alter (Miniature Excitatory Postsynaptic Current) mEPSC amplitude or frequency, but inhibits the activity-induced increase in (Excitatory Postsynaptic Current) EPSC amplitude ratio in cerebellar stellate cells^[1].

Pep2-AVKI (1 mM) blocks the increase in synaptic GluR2-containing receptors in cerebellar stellate cells^[1].

Pep2-AVKI increases AMPA-evoked (radiolabeled norepinephrine) [³H]NA and (radiolabeled D-aspartate) [³H]D-ASP and increases 10 μM NMDA/1 μM Glycine (HY-Y0966)/50 μM (S) AMPA-induced tritium release, but does not alter 10 μM NMDA/1 μM Glycine-induced [³H]D-ASP release in hippocampal synaptosomes^[2][3].

Pep2-AVKI (100 μM) blocks (Long-Term Depression) LTD in postsynaptic neurons^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1268.46

C₆₀H₉₃N₁₃O₁₇

1315378-69-8

Tyr-Asn-Val-Tyr-Gly-Ile-Glu-Ala-Val-Lys-Ile

YNVYGIEAVKI

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu SJ, et al. Subunit interaction with PICK and GRIP controls Ca2+ permeability of AMPARs at cerebellar synapses. Nat Neurosci. 2005 Jun;8(6):768-75.  [Content Brief]

  [2]. Pittaluga A, et al. Trafficking of presynaptic AMPA receptors mediating neurotransmitter release: neuronal selectivity and relationships with sensitivity to cyclothiazide. Neuropharmacology. 2006 Mar;50(3):286-96.  [Content Brief]

  [3]. Summa M, et al.Hippocampal AMPA autoreceptors positively coupled to NMDA autoreceptors traffic in a constitutive manner and undergo adaptative changes following enriched environment training. Neuropharmacology. 2011 Dec;61(8):1282-90.  [Content Brief]

  [4]. Toyoda H, et al. Long-term depression requires postsynaptic AMPA GluR2 receptor in adult mouse cingulate cortex. J Cell Physiol. 2007 May;211(2):336-43.  [Content Brief]