BMS-201620: a selective beta 3 agonist.

W N Washburn; C-Q Sun; G Bisacchi; G Wu; P T Cheng; P M Sher; D Ryono; A V Gavai; K Poss; R N Girotra; P J McCann; A B Mikkilineni; T C Dejneka; T C Wang; Z Merchant; M Morella; C M Arbeeny; T W Harper; D A Slusarchyk; S Skwish; A D Russell; G T Allen; B Tesfamariam; B H Frohlich; B E Abboa-Offei; M Cap; T L Waldron; R J George; D Young; K E Dickinson; A A Seymour

doi:10.1016/j.bmcl.2004.04.074

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PubMed · 15177466

BMS-201620: a selective beta 3 agonist.

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Abstract

A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.

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Adrenergic beta-3 Receptor Agonists Adrenergic beta-Agonists Animals Dose-Response Relationship, Drug Drug Evaluation, Preclinical Glycine Haplorhini Humans Methylation Receptors, Adrenergic, beta-3 Stereoisomerism Structure-Activity Relationship Comparative Study Journal Article

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W N Washburn, C-Q Sun, G Bisacchi, G Wu, P T Cheng, P M Sher, D Ryono, A V Gavai, K Poss, R N Girotra, P J McCann, A B Mikkilineni, T C Dejneka, T C Wang, Z Merchant, M Morella, C M Arbeeny, T W Harper, D A Slusarchyk, S Skwish, A D Russell, G T Allen, B Tesfamariam, B H Frohlich, B E Abboa-Offei, M Cap, T L Waldron, R J George, D Young, K E Dickinson, A A Seymour. 2004-07-05. BMS-201620: a selective beta 3 agonist.. https://doi.org/10.1016/j.bmcl.2004.04.074

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