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- W1574660663 abstract "The clinical utility of β3-AR agonists depends on both their efficacy and on their selectivity. The presence of significant β1- and β2-AR related side-effects has been responsible for stopping the development of several compounds and highlights the importance of optimizing β3-selectivity against human receptors. This has contributed to the subdivision of β-adrenergic receptors (β-AR) into β1- and β2-AR has led to the development of β1- and β2-AR antagonists and agonists, as well as nonselective β3-AR antagonists, that have been useful for the treatment of cardiovascular disease and asthma. A third subtype of β-AR has led to the development of β3-AR agonists that may prove useful in the treatment of various metabolic diseases. A common feature of atypical or β3-AR is that they mediate responses that are insensitive to the most standard β-AR antagonists. They are also more responsive than β1- or β2-AR to the novel agonists. The selectivity of β3-AR agonists has typically been determined by functional assays in adipocytes or colon, atrium, and trachea or uterus. More recently, a series of β3-AR agonists has been ranked by their ability to stimulate cyclic adenosine monophosphate (AMP) production in Chinese hamster ovary cells that have been transfected with the human β1-, β2-, or β3-AR. Two aryloxypropranol-aminotetralines have recently been reported to be selective antagonists for the β3-AR." @default.
- W1574660663 created "2016-06-24" @default.
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- W1574660663 date "1995-01-01" @default.
- W1574660663 modified "2023-10-03" @default.
- W1574660663 title "Chapter 20. β3-Selective Adrenergic Receptor Agonists" @default.
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- W1574660663 doi "https://doi.org/10.1016/s0065-7743(08)60933-1" @default.
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