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Type
Synthetic heptapeptide (spadin-derived fragment)
Molecular formula
C₃₅H₅₅N₁₁O₉
Molecular weight
773.89 Da
CAS number
1801959-12-5
Amino acids
7
Sequence
Gly-Val-Ser-Trp-Gly-Leu-Arg
Modification
None (linear peptide)
PE-22-28 is a selective inhibitor of the TREK-1 (KCNK2) two-pore-domain potassium channel. TREK-1 is a background K⁺ channel that contributes to stabilizing neuronal resting membrane potential; blocking it reduces this stabilization and alters cell excitability. Patch-clamp recordings in human TREK-1–expressing cell lines show that PE-22-28 inhibits TREK-1 current; comparative assays of the parent spadin peptide in the same system indicate lower inhibitory activity, motivating the truncation strategy that produced this fragment. PE-22-28's compact structure—7 residues with a hydrophobic tryptophan and a basic arginine—is structurally consistent with binding near the extracellular pore of TREK-1. In selectivity panels, PE-22-28 did not produce significant current inhibition at the closely related K2P channels TREK-2 or TRAAK. PE-22-28 is therefore characterized as a selective peptide antagonist of a neuronal two-pore K⁺ channel.
Lyophilized
–20 °C
store dry and protected from moisture.
No long-term stability data are published for this peptide; general small-peptide handling practices (sealed, dry, minimize freeze–thaw) apply.
Reviews
Djillani A, Mazella J, Heurteaux C, Borsotto M. (2019). Frontiers in Pharmacology
Borsotto M, Veyssiere J, Moha ou Maati H, Devader C, Maurin Y, et al. (2015). British Journal of Pharmacology
Reviews
Djillani A, Pietri M, Mazella J, Heurteaux C, Borsotto M. (2019). Pharmacology & Therapeutics
Mazella J, Borsotto M, Heurteaux C. (2019). Frontiers in Pharmacology
Clinical
Devader C, Roulot M, Moréno S, et al. (2017). Journal of Affective Disorders
Roulot M, Minelli A, Bortolomasi M, et al. (2018). Neuropsychiatric Disease and Treatment
Buttenschøn HN, Nielsen M, Glerup S, Mors O. (2018). Acta Neuropsychiatrica
Primary research
Daziano G, Blondeau N, Béraud-Dufour S, Abderrahmani A, Rovère C, Heurteaux C, Mazella J, Lebrun P, Coppola T. (2021). Pharmacological Research
Pietri M, Djillani A, Mazella J, Borsotto M, Heurteaux C. (2019). Neuropharmacology
Djillani A, Pietri M, Moreno S, Heurteaux C, Mazella J, Borsotto M. (2017). Frontiers in Pharmacology
Mazella J, Pétrault O, Lucas G, et al. (2010). PLoS Biology
Moha ou Maati H, Veyssière J, Labbal F, Coppola T, et al. (2012). Neuropharmacology
Veyssière J, Moha ou Maati H, Mazella J, Gaudriault G, Moreno S, Heurteaux C, Borsotto M. (2015). Psychopharmacology
Moreno S, Devader CM, Pietri M, Borsotto M, Heurteaux C, Mazella J. (2018). Frontiers in Pharmacology
Devader C, Khayachi A, Veyssière J, et al. (2015). British Journal of Pharmacology
Hivelin C, Béraud-Dufour S, Devader C, et al. (2016). Journal of Diabetes Research
Ma R, Lewis A. (2020). Frontiers in Pharmacology
Wu F, Sun H, Gong W, Li X, Pan Z, Shan H, Zhang Z. (2021). CNS Neuroscience & Therapeutics
Wang W, Kiyoshi CM, Du Y, et al. (2020). Molecular Neurobiology
Kim A, Jung HG, Kim YE, et al. (2019). International Journal of Molecular Sciences
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