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Products
Pharmacology
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- Technical support
- Resources
Spadin
Cat. No. KC-040
Structure:
H-Tyr-Ala-Pro-Leu-Pro-Arg-Trp-Ser-Gly-Pro-Ile-Gly-Val-Ser-Trp-Gly-Leu-Arg-OH
Activity:
TREK-1 channel blocker
Spadin is a natural peptide released from the maturation of neurotensin receptor 3 (also known as sortilin) which acts as a TREK-1 (TWIK-related K+ channel-1) channel blocker with an IC50 of 71 nM. In electrophysiological studies, spadin blocks the TREK-1 activity in COS-7 cells, in cultured hippocampal pyramidal neurons and CA3 hippocampal neurons in brain slices and in vivo induces an increase of the 5-HT neuron firing rate in the dorsal raphe nucleus. Spadin is brain penetrant, and exhibits antidepressant effects in mouse models of depression with a rapid onset of action and an absence of adverse effects. The antidepressant properties are associated with increased neurogenesis and synaptogenesis in the brain.
Mazella et al (2010) Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design. PLoS Biol. 8 e1000355 PMID: 20405001
Borsotto et al (2015) Targeting two-pore domain K(+) channels TREK-1 and TASK-3 for the treatment of depression: a new therapeutic concept. Br.J.Pharmacol. 172 771 PMID: 25263033
Djillani A, Pietri M, Mazella J, Heurteaux C, Borsotto M. Fighting against depression with TREK-1 blockers: Past and future. A focus on spadin. Pharmacol Ther. 194 185 PMID: 30291907
Related areas
All peptides >
All potassium channel modulators >
All neuroscience research categories >
Technical Data
| Structure | H-Tyr-Ala-Pro-Leu-Pro-Arg-Trp-Ser-Gly-Pro-Ile-Gly-Val-Ser-Trp-Gly-Leu-Arg-OH |
| CAS Number | 1270083-24-3 |
| Molecular Weight | 2012.34 |
| Formula | C96H142N26O22 |
| Sequence | YAPLPRWSGPIGVSWGLR |
| Modifications | None |
Solubility and Storage
| Solubility | Soluble to 2 mg/ml in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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