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2005
Receptor binding activity
X 0280
Discovery of a Novel and Potent Human and Rat β3-Adrenergic Receptor Agonist,
33- 280 [3-[(2R)-[[(2R)-(3-Chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic Acid. — In search for potent and selective β3-adrenergic receptor
(β3-AR) agonists as potential drugs for the treatment of type II diabetes and obesity, the
title compound (I) and a series of structurally related substances such as (II) are synthesized and tested for their biological activity at human β1-, β2-, and β3-ARs as well
as at rat β3-AR expressed in Chinese hamster ovary (CHO) cells. The absolute configuration of (I) is confirmed by single-crystal X-ray analysis. On the basis of its promising pharmacological profile, compound (I) is in clinical development. —
(HARADA*, H.; HIROKAWA, Y.; SUZUKI, K.; HIYAMA, Y.; OUE, M.;
KAWASHIMA, H.; KATO, H.; YOSHIDA, N.; FURUTANI, Y.; KATO, S.; Chem.
Pharm. Bull. 53 (2005) 2, 184-198; Chem. Res. Lab., Dainippon Pharm. Co., Ltd.,
Suita, Osaka 564, Japan; Eng.) — H. Haber
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