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Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC 50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and
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In Vitro:Spadin TFA (100 nM; COS-7 cells) has inhibitory effect of spadin on the TREK-1 channel and blocks 63% of the TREK-1 current stimulated by arachidonic acid. Spadin TFA (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain sl
In Vivo:Spadin TFA (10 μM, 100 μL; 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). Spadin TFA (0.01-100 μM, 100 μL; ICV, i.p. and i.v.; daily, for 7 days; male C57Bl/6J an
Biological Activity:Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC 50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and