Biological ActivityPotent TREK-1 channel blocker (IC 50 = 71 nM). Enhances dorsal raphe nucleus 5-HT neurotransmission in mice. Induces hippocampal CREB activation and neurogenesis in adult mice. Exhibits antidepressant effects in mouse models of depression. Brain penetrant.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design.
Mazella et al.
PLoS Biol., 2010;8:e1000355
Targeting two-pore domain K(+) channels TREK-1 and TASK-3 for the treatment of depression: a new therapeutic concept.
Borsotto et al.
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A very potent K2p channel blocker which was used to figure out the blocking activity as concentration of the blocker molecule increased. Spadin is a great antagonist molecule which shows channel blocking properties which is concentration dependent.