Title : Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes.

Pub. Date : 1989 Nov 28

PMID : 2606156






2 Functional Relationships(s)
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1 In vitro, THA inhibits acetylcholinesterase (AChE) (IC50 = 223 nM) and blocks [3H]AFDX-116 (M2) and [3H]telenzepine (M1) binding (IC50 s of 1.5 and 9.1 microM respectively). Tacrine acetylcholinesterase Rattus norvegicus
2 We conclude that brain AChE inhibition by THA is sufficient to explain its purported therapeutic activity in Alzheimer"s disease and that its favorable brain/plasma distribution in vivo may account for its central cholinergic action without inducing the severe peripheral cholinergic effects typically seen with other AChE inhibitors. Tacrine acetylcholinesterase Rattus norvegicus