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855291-54-2

855291-54-2 Structure

855291-54-2 Structure
IdentificationBack Directory
[Name]

ABT 107)
[CAS]

855291-54-2
[Synonyms]

ABT 107)
ABT-107 (ABT107
(R)-3-((6-(1H-Indol-5-yl)pyridazin-3-yl)oxy)quinuclidine
1-Azabicyclo[2.2.2]octane, 3-[[6-(1H-indol-5-yl)-3-pyridazinyl]oxy]-, (3R)-
[Molecular Formula]

C19H20N4O
[MOL File]

855291-54-2.mol
[Molecular Weight]

320.39
Chemical PropertiesBack Directory
[Boiling point ]

598.0±50.0 °C(Predicted)
[density ]

1.33±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

16.01±0.30(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

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].
[in vivo]

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].

Animal Model:Rats (male Sprague-Dawley; 350-380 g b.wt.)[1].
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[1].
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.
[References]

[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. DOI:10.1124/jpet.110.167213
[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. DOI:10.1016/j.expneurol.2014.09.015
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