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

Authors: Sawa, Masaaki; Harada, Hiroshi

Source: Current Medicinal Chemistry, Volume 13, Number 1, January 2006 , pp. 25-37(13)

Publisher: Bentham Science Publishers

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Abstract:

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

Document Type: Research article

Affiliations: 1: Chemistry Research Laboratories, Drug Research Division, Dainippon Sumitomo Pharma Co., Ltd., 33-94 Enoki-cho, Suita, Osaka 564-0053, Japan;

Publication date: 2006-01-01

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Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.