143285-75-0Relevant articles and documents
Synthesis and binding to β-adrenergic receptors of p-aminobenzyl analogues of practolol and atenolol
Jones Jr.,Bylund,Hanson
, p. 397 - 398 (2007/10/02)
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 β1-adrenergic receptors), the affinities of the derivatives and parent compounds were similar. By contrast, in membranes from the lung (which contain mostly β2-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.
