ABT-107 is a selective α7 neuronal nicotinic receptor agonist. ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions.
体内研究
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.
ABT-107 (0.01-1 μmol/kg i.p., 15 min before sacrifice) produces a dose-dependent increase in ERK1/2 and CREB.
ABT-107 (0.01, 0.1, and 1.0 mg/kg i.p.) increases S-GSK3 and decreases p-tau in mouse cortex and hippocampus in mice.
ABT-107 (5 mg/kg/day i.p.) infusion attenuates tau hyperphosphorylation in AD transgenic APP-tau mice.
Animal Model:
Rats (male Sprague-Dawley; 350-380 g b.wt.).
Dosage:
1, 3 μmol/kg.
Administration:
I.P. daily for 3 consecutive days.
Result:
Induced a significant, dose-dependent increase in ACh release by day 3 of repeated administration.
Higher doses may be required to evoke ACh release in naive rats not engaged in stimulated, i.e., cognitive-related behavior.
Animal Model:
Female TAPP (and wild-type littermates) mice.
Dosage:
1 mg/kg.
Administration:
Continuous subcutaneous infusion for 2 weeks.
Result:
Produced a dose-dependent increase in Ser9 phosphorylation in the cingulate cortex 15 min after acute administration in mice.
分子式
C19H20N4O
分子量
320.39
CAS号
855291-54-2
运输条件
Room temperature in continental US; may vary elsewhere.