.beta.1-Selective adrenoceptor antagonists. 2. 4-Ether-linked phenoxypropanolamines
- 1 November 1983
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 26 (11) , 1570-1576
- https://doi.org/10.1021/jm00365a005
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 1000 times greater. The compounds also possessed partial agonist activity in rats. Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on .beta.-adrenoceptors. [The use of .beta.-adrenoceptor antagonists is now widely established in the treatment of essential hypertension.].This publication has 8 references indexed in Scilit:
- .beta.1-Selective adrenoceptor antagonists. 1. Synthesis and .beta.-adrenergic blocking activity of a series of binary (aryloxy)propanolaminesJournal of Medicinal Chemistry, 1983
- Effects of fluorine analogs of norepinephrine on stimulation of cyclic adenosine 3′,5′- monophosphate and binding to β-adrenergic receptors in intact pinealocytesBiochemical Pharmacology, 1981
- Aromatic hydroxylation of .beta.-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-(allyloxy)phenoxy]-2-propanol from oxprenololJournal of Medicinal Chemistry, 1979
- Cardioselectivity as a function of molecular structure in .beta.-adrenoceptor blocking agents of the 1-(para-substituted aryloxy)-3-(isopropylamino)propan-2-ol typeJournal of Medicinal Chemistry, 1978
- Pamatolol: Phase I evaluation of the pharmacodynamics of a cardioselective beta adrenoceptor blocking drugClinical Pharmacology & Therapeutics, 1978
- .beta.-Adrenergic blocking agents. 16. 1-(Acylaminomethyl-, ureidomethyl-, and ureidoethylphenoxy)-3-amino-2-propanolsJournal of Medicinal Chemistry, 1977
- .beta.-Adrenergic blocking agents. 15. 1-Substituted ureidophenoxy-3-amino-2-propanolsJournal of Medicinal Chemistry, 1977
- SELECTIVE BLOCKADE OF ADRENOCEPTIVE BETA RECEPTORS IN THE HEARTBritish Journal of Pharmacology, 1968