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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists

Author(s): Masaaki Sawa and Hiroshi Harada

Volume 13 , Issue 1 , 2006

Page: [25 - 37] Pages: 13

DOI: 10.2174/092986706775198006

Price: $65


The β3-adrenergic receptor (β3-AR) has been shown to mediate various pharmacological and physiological effects such as lipolysis, thermogenesis, and relaxation of the urinary bladder. Activation of the β3-AR is thought to be a possible approach for the treatment of obesity, type 2 diabetes mellitus, and frequent urination. Therefore, the β3-AR is recognized as an attractive target for drug discovery. On the other hand, activation of the β1- or β2-AR can cause undesirable side effects such as increased heart rate or muscle tremors. Consequently, a number of recent efforts in this field have been directed toward the design of selective agonists for the β3-AR. This review summarizes recent advances in β3-AR agonists with an emphasis on recent attempts to create potent, selective and orally bioavailable small-molecule agonists.

Keywords: β3-adrenergic receptor, G protein-coupled receptor, agonist, obesity, type2 diabetes mellitus, frequent urination, lipolysis, thermogenesis

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