α7 nAChR partial agonist
A 844606 is a potent and selective partial agonist of α7 nicotinic acetylcholine receptor (nAChR) with IC50 value of 11 nM [1].
The α7 nAChR is a nicotinic acetylcholine receptor and is located in the brain, spleen and lymphocytes of lymph nodes. The α7 nAChR plays an important role in the pathophysiology of neuropsychiatric diseases such as Alzheimer’s disease, schizophrenia, drug addiction and depression [2].
A 844606 is a potent and selective α7 nAChR partial agonist with IC50 values of 11 and >30000 nM for α7 and α4β2, respectively. In Xenopus oocytes expressed recombinant human and rat α7 nAChR, A 844606 showed agonist activity with EC50 values of 1.4 and 2.2 μM, respectively. In PC12 cells, A 844606 activated α7 nAChR, which stimulated ERK1/2 phosphorylation [1].
In the mouse brain, A 844606 showed high uptake. In monkey brain, A 844606 was mainly distributed in the thalamus and hippocampus and was low in the cerebellum. Also, A 844606 was reduced by pretreatment with SSR180711, an α7 nAChR agonist [2].
参考文献:
[1].? Briggs CA, Schrimpf MR, Anderson DJ, et al. alpha7 nicotinic acetylcholine receptor agonist properties of tilorone and related tricyclic analogues. Br J Pharmacol, 2008, 153(5): 1054-1061.
[2].? Toyohara J, Ishiwata K, Sakata M, et al. In vivo evaluation of alpha7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys. PLoS One, 2010, 5(2): e8961.
动态评分
0.0