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2005
Receptor binding activity
X 0280
Tryptamine-Based Human β3-Adrenergic Receptor Agonists. Part 1. SAR Studies
the 7-Position of the Indole Ring. — The title agonists are prepared by a conver15- 244 of
gent route coupling tryptamine derivatives with a sulfonamide. The triptamine-based arylsulfonamide compounds possessing alkyloxy or sulfonate groups at the
7-position of the indole ring are evaluated with respect to their agonistic activity for the
β1-3 adrenergic receptors. Methanesulfonate (I) is a highly potent β3-AR agonist with
excellent subtype selectivity over the β1- and β2-ARs. — (MIZUNO*, K.;
SAWA, M.; HARADA, H.; TATEISHI, H.; OUE, M.; TSUJIUCHI, H.; FURUTANI,
Y.; KATO, S.; Bioorg. Med. Chem. Lett. 14 (2004) 24, 5959-5962; Chem. Res. Lab.,
Dainippon Pharm. Co., Ltd., Suita, Osaka 564, Japan; Eng.) — H. Hoennerscheid
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