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产品价格:电议      采购度:1181      原产地:美洲
发布时间:2022/9/29 9:05:37 所属地区:国外 国外
简要描述:
N-Salicyloyltryptamine 是一种电压依赖性离子通道抑制剂,包括 Na+、Ca2+、K+ 通道。N-Salicyloyltryptamine 抑制 K+ 电流的 IC50 为 μM (Ito)。N-Salicyloyltryptamine 还具有抗惊厥、抗炎、镇痛,和血管舒张的作用。
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CAS No. : 31384-98-2
MCE 站:N-Salicyloyltryptamine
产品活性:N-Salicyloyltryptamine 是一种电压依赖性离子通道抑制剂,包括 Na+、Ca2+、K+ 通道。N-Salicyloyltryptamine 抑制 K+ 电流的 IC50 为 34.6 μM (Ito)。N-Salicyloyltryptamine 还具有抗惊厥、抗炎、镇痛,和血管舒张的作用。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling | MAPK/ERK Pathway | Stem Cell/Wnt | GPCR/G Protein | NF-κB
作用靶点:Calcium Channel | ERK | Potassium Channel | Guanylate Cyclase | NF-κB
In Vitro: 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 M) produces vasorelaxation through activation of the NO/sGC/cGMP pathway and reduction of calcium influx.
In Vivo: 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.
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更新时间:2024/1/2 10:26:55
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