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Synthesis and muscarinic M3 pharmacological activities of 1-azabicyclo[2.2.2]octan-3-one oxime derivatives

✍ Scribed by Ralf Plate; Marc J.M. Plaum; Thijs de Boer; John S. Andrews

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 634 KB
Volume: 4
Category: Article
ISSN: 0968-0896
DOI: 10.1016/0968-0896(96)00035-1

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✦ Synopsis

A series of 1-azabicyclo[2.2.2]octan-3-one oximes and related 1-azabicyclo-[2.2.2]-octan-3-one hydroxylamines were synthesized and tested for muscarinic M3 activity. All compounds showed at least some muscarinic binding properties, however, only one member of the series demonstrated mucarinic M3 agonistic properties in vitro (contraction of guinea pig ileum) and in vivo (mydriasis, salivation). In addition, this compound partially reversed the cognitive deficit induced by central cholinergic depletion in two procedures testing memory in the rat, namely the delayed matching to position and swim maze tasks of spatial memory in the rat.

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