Spadin peptide

Spadin peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

H-YAPLPRWSGPIGVSWGLR-OH

H-Tyr-Ala-Pro-Leu-Pro-Arg-Trp-Ser-Gly-Pro-Ile-Gly-Val-Ser-Trp-Gly-Leu-Arg-OH

18

95.23%

C₉₆H₁₄₂N₂₆O₂₂

2012.31

Synthetic

Powder

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.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• 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

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.