ABT-107 是选择性的 α7 神经元尼古丁受体的激动剂。ABT-107 对单侧 6-羟多巴胺损伤大鼠的黑质纹状体损伤起到保护作用。
ABT-107 is a selective α7 neuronal nicotinic receptor agonist. ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions[1][2].
ABT-107 exhibits good bioavailability in mouse (orally, 51.1%; intraperitoneally,100%), rat (orally, 81.2%; intraperitoneally, 100.0%), and monkey (orally, 40.6%; intramuscularly, 100%), and good CNS penetration in rodents with a brain/plasma ratio of 1[1].ABT-107 (0.01-1 μmol/kg i.p., 15 min before sacrifice) produces a dose-dependent increase in ERK1/2 and CREB[1]. ABT-107 (0.01, 0.1, and 1.0 mg/kg i.p.) increases S9-GSK3 and decreases p-tau in mouse cortex and hippocampus in mice[1].ABT-107 (5 mg/kg/day i.p.) infusion attenuates tau hyperphosphorylation in AD transgenic APP-tau mice[1].
[1]. R Scott Bitner, et al. In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer’s disease. J Pharmacol Exp Ther. 2010 Sep 1;334(3):875-86.
[2]. Tanuja Bordia, et al. The α7 nicotinic receptor agonist ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions. Exp Neurol. 2015 Jan;263:277-84.
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