title: Studies on cognitive enhancing agents. II. Antiamnestic and antihypoxic activities of 1-aryl-2-(2-aminoethoxy)ethanols.
abstract: A series of 2-(2-aminoethoxy)-1-phenylethanols having a variety of N- and phenyl-substitution patterns as well as 5- and 6-membered heteroaryl counterparts of our prototype compound 1 (2-(2-dimethylaminoethoxy)-1-phenylethanol) have been prepared and evaluated for antiamnestic and antihypoxic activities. Compound 3b, the 3-methylphenyl analogue of 1, proved to be significantly more potent than 1 in reversing electroconvulsive shock-induced amnesia as well as CO2-induced learning-impairment in mice. It exhibited low acute toxicity in mice and afforded a greater brain/serum concentration ratio than 1 after oral administration to rats.
authors.affiliation: Research Laboratories, Toyama Chemical Co., Ltd., Japan.
authors.forename: S
authors.initials: S
authors.lastname: Ono
authors.forename: T
authors.initials: T
authors.lastname: Yamafuji
authors.forename: H
authors.initials: H
authors.lastname: Chaki
authors.forename: H
authors.initials: H
authors.lastname: Morita
authors.forename: Y
authors.initials: Y
authors.lastname: Todo
authors.forename: M
authors.initials: M
authors.lastname: Maekawa
authors.forename: K
authors.initials: K
authors.lastname: Kitamura
authors.forename: M
authors.initials: M
authors.lastname: Tai
authors.forename: H
authors.initials: H
authors.lastname: Narita
mesh_terms: D000647:Amnesia / Q000188:drug therapy* / Q000523:psychology; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001812:Blood-Brain Barrier; D003460:Crystallization; D004597:Electroshock; D000431:Ethanol / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002534:Hypoxia, Brain / Q000188:drug therapy* / Q000523:psychology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar
chemical_list: D018697:Nootropic Agents; D000431:Ethanol