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编 号:F315999
分子式:C17H16N2O2
分子量:280.32
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5mg
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10mg
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生物活性:
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect-.

体内研究:
N-Salicyloyltryptamine (100 mg/kg; i.p.; 60 min before stimulation challenge) significantly inhibits pentylenetetrazol (PTZ)-induced seizures and partially eliminates the extensor reflex of maximal electric-induced seizures test.N-Salicyloyltryptamine (100 mg/kg, 200 mg/kg; i.p.; single dose) shows antinociceptive and nerve excitability effects.Animal Model:Male Swiss mice (25-35 g)
Dosage:50, 100, 200 mg/kg
Administration:Intraperitoneal injection; single dose; 60 min before stimulation challenge
Result:Reduced the incidence of clonic pentylenetetrazol (PTZ) seizures and mortality at 50 mg/kg, and decreased the incidence of tonic hindlimb extension (THE) produced by MES at 100, 200 mg/kg.
Animal Model:Male Swiss mice (25-35 g)
Dosage:100 mg/kg; 200 mg/kg
Administration:Intraperitoneal injection; single dose
Result:Reduced the acetic acid-induced licking response of the injected paw.

体外研究:
N-Salicyloyltryptamine (1 ng/mL-1 μg/mL; 24 h) presents no cytotoxicity and causes no oxidative stress in RAW 264.7 cells at low concentration, but (50 and 100 μg/mL) inhibits cell viability with an IC50 value of 22.75 μg/mL.N-Salicyloyltryptamine (1 μg/mL; 24 h) reverses some redox and inflammatory parameters induced by LPS without interfering in cell viability.N-Salicyloyltryptamine (1 μg/mL; 24 h) inhibits LPS-induced TNF-α and IL-1β release, as well as CD40 and TNF-α protein up-regulation.N-Salicyloyltryptamine (1 μg/mL; 24 h) inhibits phosphorylation of ERK 1/2 and IκBα and p65 nuclear translocation (NF-kB activation).N-Salicyloyltryptamine (17 μM) inhibits K+ current by 59.27% (Ito) and 73.18% (IKD), inhibits L-type Ca2+ currents by 54.9%, and shows few inhibition with high concentration (170 μM) on TTX-sensitive Na+ current by 22.1% in GH3 cells.N-Salicyloyltryptamine (0.01 nM-100 μM) produces vasorelaxation through activation of the NO/sGC/cGMP pathway and reduction of calcium influx.
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