Amodiaquine在人红细胞中是一种有效的、非竞争性的组胺N-甲基转移酶抑制剂,其Ki值为18.6 nM。它也被用作抗疟疾药和消炎药。
Target | Value |
histamine N-methyl transferase
(Cell-free assay)
|
18.6 nM(Ki)
|
Amodiaquine (10-20 μM; 4 hours) treatment suppresses LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
Amodiaquine (5 μM; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primary dopamine cells as examined by the number of TH
+
neurons and dopamine uptake. The neuroprotective effect of Amodiaquine is also observed in rat PC12 cells.
RT-PCR
Cell Line:
|
Primary microglia
|
Concentration:
|
10 µM, 15 µM, 20 µM
|
Incubation Time:
|
4 hours
|
Result:
|
Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
|
在狗的体内实验中,小剂量的amodiaquine显著地增强了组胺对胃液分泌的作用。对 P. acnes-primed和LPS诱导的肝炎小鼠中,处理以amodiaquine,能有效阻止严重肝损伤和高致死性,增强了组胺的升高而不升高tele-methylhistamine (t-MeHA)。
用途
用作抗疟药