| Identification | Back Directory | [Name]
SPADIN | [CAS]
1270083-24-3 | [Synonyms]
SPADIN
PubChem ID: 91826106
L-Arginine, L-tyrosyl-L-alanyl-L-prolyl-L-leucyl-L-prolyl-L-arginyl-L-tryptophyl-L-serylglycyl-L-prolyl-L-isoleucylglycyl-L-valyl-L-seryl-L-tryptophylglycyl-L-leucyl- | [Molecular Formula]
C96H142N26O22 | [MDL Number]
MFCD30182326 | [MOL File]
1270083-24-3.mol | [Molecular Weight]
2012.32 |
| Chemical Properties | Back Directory | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 2 mg/ml in H2O | [form ]
solid | [pka]
3.34±0.10(Predicted) | [color ]
White | [Water Solubility ]
Soluble in water (1 mg/ml) |
| Hazard Information | Back Directory | [Uses]
Spadin is an anti-depressant molecule that blocks TREK-1 potassium channels. | [Biological Activity]
spadin is a potent trek-1 channel inhibitor with ic50 of 71nm. it is a secreted peptide derived from the propeptide generated by the maturation of ntsr3/sortilin. [1]trek-1, aka kcnk2, is a two-pore domain ion channel that involved in the passive transmembrane k+ transport. it is related to the ischemia, anesthesia and electrogenesis in the neurons. it also plays an important role in the pathophysiological process of depression and in the response to antidepressant. [1]in trek-1 transfected cos-7 cells, 100nm of spadin inhibited 63% of the trek-1 current stimulated by arachidnice acid. spadin also blocked the trek-1 channels activity in ca3 hippocampal neurons on brain slices of wild-type mice. [1]in behavioral tests that predicting an antidepressant response, spadin-treated mice displayed a resistance to depression. mice treated with spadin for 4 days also exhibited a significant antidepressant effect as well as elevated hippocampal phosphorylation of creb protein and neurogenesis. [2] | [in vivo]
Spadin (10 μM; i.p.; for 30 min; male C57Bl/6J and TREK-1 deficient mice) increases of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN)[2].
Spadin (0.01-100 μM; ICV, i.p. and i.v.; daily, for 7 days; male C57Bl/6J and TREK-1 deficient mice) has anti-depressant behavior in mice[2]. | Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | | Dosage: | 10 μM | | Administration: | Intraperitoneal injection; for 30 min | | Result: | Increased of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN). |
| Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | | Dosage: | 0.01-100 μM | | Administration: | Intracerebroventrical injection, intraperitoneal injection and intravenous injection; daily, for 7 days | | Result: | Had any effect on mouse locomotion analyzed in short- or long-time after the drug injection. |
| [storage]
Store at -20°C | [References]
1. borsotto m, veyssiere j, moha ou maati h et al. targeting two-pore domain k(+) channels trek-1 and task-3 for the treatment of depression: a new therapeutic concept. br j pharmacol. 2015 feb;172(3):771-84.2. mazella j, pétrault o, lucas g, et al. spadin, a sortilin-derived peptide, targeting rodent trek-1 channels: a new concept in the antidepressant drug design. plos biol. 2010 apr 13;8(4):e1000355. |
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