Abstract
The synthesis and SAR of a series of human beta3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human beta3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
MeSH terms
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Adrenergic beta-3 Receptor Agonists*
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Adrenergic beta-Agonists / chemical synthesis*
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Adrenergic beta-Agonists / pharmacology*
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Animals
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CHO Cells
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Cricetinae
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Humans
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Indicators and Reagents
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Mice
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Mice, Transgenic
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Receptors, Adrenergic, beta-3 / genetics
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Structure-Activity Relationship
Substances
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Adrenergic beta-3 Receptor Agonists
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Adrenergic beta-Agonists
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Indicators and Reagents
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Piperidines
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Receptors, Adrenergic, beta-3