Title of article
4-Aminopiperidine ureas as potent selective agonists of the human β3-Adrenergic receptor
Author/Authors
Mark A. Ashwell، نويسنده , , William R. Solvibile Jr.، نويسنده , , Stella Han، نويسنده , , Elwood Largis، نويسنده , , Ruth Mulvey، نويسنده , , Jeffrey Tillet، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
5
From page
3123
To page
3127
Abstract
The preparation and structure–activity relationships (SARs) of potent agonists of the human β3-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human β3-AR potency with selectivity over human β1-AR and/or human β2-AR agonism. Compound 29s was identified as a potent (EC50=1 nM) and selective (greater than 400-fold over β1- with no β2-AR agonism) full β3-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791807
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