Synthesis and binding to beta-adrenergic receptors of p-aminobenzyl analogues of practolol and atenolol
| Autor: | Robert N. Hanson, Gerald S. Jones, David B. Bylund |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
Adrenergic receptor
Chemistry Stereochemistry Myocardium Adrenergic beta-Antagonists Pharmaceutical Science Pharmacology Atenolol In vitro Rats Dissociation constant Membrane Adrenergic receptor antagonists Receptors Adrenergic beta medicine Animals β adrenergic receptor Practolol Lung medicine.drug |
| Zdroj: | Journal of pharmaceutical sciences. 81(4) |
| ISSN: | 0022-3549 |
| Popis: | The p ‐aminobenzyl analogues ( 8a and 8b , respectively) of the cardioselective β ‐adrenergic receptor antagonists practolol and atenolol were prepared from the corresponding phenoxymethyloxiranes in 30 and 13% yields, respectively. The dissociation constants for the β ‐adrenergic receptor were measured in membrane preparations of rat heart and lung, in membranes from the heart (which contain mostly β 1 ‐adrenergic receptors), the affinities of the derivatives and parent compounds were similar. By contrast, in membranes from the lung (which contain mostly β 2 ‐adrenergic receptors), the derivatives were more potent than the parent compounds. Thus, the cardioselectivities of the p ‐aminobenzyl analogues 8a and 8b were about one‐sixth those of the respective parents. |
| Databáze: | OpenAIRE |
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