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编 号:F555328
分子式:C96H142N26O22
分子量:2012.34
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Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.

体内研究:
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).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.Animal Model:Male C57Bl/6J and TREK-1 deficient mice
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
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.

体外研究:
Spadin (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 (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice.
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