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Review
, 13 (1), 25-37

Recent Developments in the Design of Orally Bioavailable beta3-adrenergic Receptor Agonists

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  • PMID: 16457637
Review

Recent Developments in the Design of Orally Bioavailable beta3-adrenergic Receptor Agonists

Masaaki Sawa et al. Curr Med Chem.

Abstract

The beta3-adrenergic receptor (beta3-AR) has been shown to mediate various pharmacological and physiological effects such as lipolysis, thermogenesis, and relaxation of the urinary bladder. Activation of the beta3-AR is thought to be a possible approach for the treatment of obesity, type 2 diabetes mellitus, and frequent urination. Therefore, the beta3-AR is recognized as an attractive target for drug discovery. On the other hand, activation of the beta1- or beta2-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 beta3-AR. This review summarizes recent advances in beta3-AR agonists with an emphasis on recent attempts to create potent, selective and orally bioavailable small-molecule agonists.

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