N-Salicyloyltryptamine(STP) is a tryptamine analogue with anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect. N-Salicyloyltryptamine acts as the voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor which inhibits K + currents with an IC 50 value of 34.6 μM ( /to) [1] - [5].
体外活性
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 IC 50 value of 22.75 μg/mL [1]. N-Salicyloyltryptamine (1 μg/mL; 24 h) reverses some redox and inflammatory parameters induced by LPS without interfering in cell viability [1]. 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 [1]. N-Salicyloyltryptamine (1 μg/mL; 24 h) inhibits phosphorylation of ERK 1/2 and IκBα and p65 nuclear translocation (NF-kB activation) [1]. N-Salicyloyltryptamine (17 μM) inhibits K + current by 59.27% ( I to ) and 73.18% ( I KD ), inhibits L-type Ca 2+ currents by 54.9%, and shows few inhibition with high concentration (170 μM) on TTX-sensitive Na + current by 22.1% in GH3 cells [2]. N-Salicyloyltryptamine (0.01 nM-100 μM) produces vasorelaxation through activation of the NO/sGC/cGMP pathway and reduction of calcium influx [3]. Cell Viability Assay [1] Cell Line: RAW 264.7 cell Concentration: 0.001, 0.05, 1, 50, 100 μg/mL Incubation Time: 24 hours Result: Resulted no effect on RAW 264.7 cell viability at 1 μg/mL; however, concentrations of 50 and 100 μg/mL significantly decreased both MTT reduction and SRB incorporation. RT-PCR [1] Cell Line: RAW 264.7 cell Concentration: 1 μg/mL Incubation Time: 24 hours Result: Reduced CD40, TNF-α, and RAGE immunocontent. Inhibited ERK1/2 and IκBα phosphorylation and nuclear translocation of p65.
体内活性
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 [4]. N-Salicyloyltryptamine (100 mg/kg, 200 mg/kg; i.p.; single dose) shows antinociceptive and nerve excitability effects [5]. Animal Model: Male Swiss mice (25-35 g) [4] 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) [5] Dosage: 100 mg/kg; 200 mg/kg Administration: Intraperitoneal injection; single dose Result: Reduced the acetic acid-induced licking response of the injected paw.
