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PubMed · 6138435

beta 1-selective adrenoceptor antagonists. 2. 4-ether-linked phenoxypropanolamines.

P J Machin·D N Hurst·R M Bradshaw·L C Blaber·D T Burden·A D Fryer·R A Melarange·C Shivdasani
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Abstract

A series of 4-substituted phenoxypropanolamines was prepared and examined for beta-adrenoceptor activity. Some of the compounds, especially the [4-[2-[[2-(4-fluorophenyl)ethyl] oxy]ethoxy]phenoxy]propanolamines (14, 15, and 24), showed potent beta 1-blockade with virtually no beta 2-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 beta-adrenoceptors.

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Adrenergic beta-AgonistsAnimalsBiological AssayBlood PressureHeart RateIndicators and ReagentsIsoproterenolMagnetic Resonance SpectroscopyPhenyl EthersPropanolaminesRatsStructure-Activity RelationshipJournal Article

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P J Machin, D N Hurst, R M Bradshaw, L C Blaber, D T Burden, A D Fryer, R A Melarange, C Shivdasani. 1983. beta 1-selective adrenoceptor antagonists. 2. 4-ether-linked phenoxypropanolamines.. https://doi.org/10.1021/jm00365a005

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Adrenergic beta-Agonists↗
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