PE 22-28 is a potent inhibitor of the TREK-1 potassium channel. This 7-amino-acid peptide is a synthetic derivative of the naturally occurring peptide spadin, which is derived from sortilin and acts as an antagonist of the TREK-1 receptor.
TREK-1 is a two-pore potassium channel found in brain regions controlling mood, memory, and learning, and is implicated in depression, neurogenesis, and synaptic plasticity. PE 22-28 has been shown to exhibit improved stability, enhanced antidepressant activity, and superior neurogenic properties compared to spadin.
Research indicates that PE 22-28 can significantly reduce depression-like symptoms in mice within four days, without the side effects associated with traditional antidepressants. Additionally, PE 22-28 has demonstrated potential in post-stroke depression, learning, stroke recovery, and neurodegenerative diseases such as Alzheimer’s. Its ability to induce neurogenesis and synaptogenesis in the hippocampus further underscores its therapeutic promise.
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| Other Names | PE 22-28, EX-A8193F, HY-P3581 |
|---|---|
| IUPAC Name | (2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid |
| CAS | 1801959-12-5 |
| Molecular Weight | 773.9 |
| Molecular Formula | C35H55N11O9 |
| SMILES | CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)CNC(=O)[C@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)CN |