Abstract
A series of 4-substituted phenoxypropanolamines was prepared and examined for β-adrenoceptor activity. Some of the compounds, especially the [4-[2-[[2-(4-fluorophenyl)ethyl]oxy]ethoxy]phenoxy]propanolamines (14,15, and 24), showed potent β1-blockade with virtually no β2-blockade at doses over a 1000 times greater. The compounds also possessed partial agonist activity. Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on β-adrenoceptors.
Original language | English (US) |
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Pages (from-to) | 1570-1576 |
Number of pages | 7 |
Journal | Journal of Medicinal Chemistry |
Volume | 26 |
Issue number | 11 |
DOIs | |
State | Published - Nov 1983 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery