Studies on cognitive enhancing agents. II. Antiamnestic and antihypoxic activities of 1-aryl-2-(2-aminoethoxy)ethanols
| Autor: | Yozo Todo, Masaru Tai, Mutsuko Maekawa, Hirokazu Narita, Satoshi Ono, Hajime Morita, Tetsuo Yamafuji, Kazunori Kitamura, Hisaaki Chaki |
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| Rok vydání: | 1995 |
| Předmět: |
Male
Stereochemistry Amnesia Mice Inbred Strains Chemical synthesis Lethal Dose 50 chemistry.chemical_compound Mice Pharmacokinetics Oral administration Drug Discovery medicine Avoidance Learning Animals Rats Wistar Hypoxia Brain Nootropic Agents Electroshock Ethanol Aryl General Chemistry General Medicine Acute toxicity Rats chemistry Blood-Brain Barrier Tacrine Toxicity medicine.symptom Crystallization medicine.drug |
| Zdroj: | Chemicalpharmaceutical bulletin. 43(9) |
| ISSN: | 0009-2363 |
| Popis: | 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 eelctroconvulsive 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. |
| Databáze: | OpenAIRE |
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