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BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Dec 03; Vol. 11 (23), pp. 3041-4. - Publication Year :
- 2001
-
Abstract
- A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(3) full agonist (K(i)=21 nM, 95% activation) with partial agonist (45%) activity at the beta(1) receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.
- Subjects :
- Administration, Oral
Adrenergic beta-1 Receptor Agonists
Animals
Blood Glucose metabolism
Chlorocebus aethiops
Drug Evaluation, Preclinical
Fatty Acids blood
Humans
Mice
Mice, Obese
Receptors, Adrenergic, beta-1 metabolism
Receptors, Adrenergic, beta-3 metabolism
Structure-Activity Relationship
Adrenergic Agonists chemistry
Adrenergic Agonists pharmacology
Adrenergic beta-3 Receptor Agonists
Anilides chemistry
Anilides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 11
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11714606
- Full Text :
- https://doi.org/10.1016/s0960-894x(01)00629-1