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- W1985366863 endingPage "398" @default.
- W1985366863 startingPage "385" @default.
- W1985366863 abstract "β3-adrenoceptors mediate some of the effects of catecholamines on tissues such as blood vessels or the urinary bladder and are putative targets for the treatment of diseases such as the overactive bladder syndrome. Progress in the understanding of the presence, function, and regulation of β3-adrenoceptors has been hampered by a lack of highly specific tools. “Classical” β3-adrenoceptor agonists such as BRL 37,344 [(R*, R*)-(±)-4[2-[(3-chlorophenyl)-2-hydroxyethyl) amino] propyl] phenoxyacetic acid] and CGP 12,177 [(±)-4-(3-t-butylamino-2-hydroxypropoxy)benzimidazol-2-one] are only partial agonists in many settings, have limited selectivity over other β-adrenoceptor subtypes, and may additionally act on receptors other than β-adrenoceptors. More efficacious and more selective agonists have been reported and, in some cases, are in clinical development but are not widely available for experimental studies. The widely used antagonist SR 59,230 [3-(2-ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanoloxalate] is not selective for β3-adrenoceptors, at least in humans, and may actually be a partial agonist. Radioligands, which are suitable either for the selective labeling of β3-adrenoceptors or for the nonselective labeling of all β-adrenoceptor subtypes, are also missing. β3- and β1/β2 double knockout mice have been reported, but their usefulness for extrapolations in humans is questionable based upon major differences between humans and rodents with regard to the ligand recognition and expression profiles of β3-adrenoceptors. While the common availability of more selective agonists and antagonists at the β3-adrenoceptor is urgently awaited, the limitations of the currently available tools need to be considered in studies of β3-adrenoceptor for the time being." @default.
- W1985366863 created "2016-06-24" @default.
- W1985366863 creator A5040869371 @default.
- W1985366863 creator A5056725548 @default.
- W1985366863 date "2007-01-09" @default.
- W1985366863 modified "2023-09-26" @default.
- W1985366863 title "Tools to study β3-adrenoceptors" @default.
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