Title of article :
Tryptamine-based human β3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring
Author/Authors :
Kazuhiro Mizuno، نويسنده , , Masaaki Sawa، نويسنده , , Hiroshi Harada، نويسنده , , Hirotaka Tateishi، نويسنده , , Mayumi Oue، نويسنده , , Hiroshi Tsujiuchi، نويسنده , , Yasuji Furutani، نويسنده , , Shiro Kato، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Abstract :
A series of tryptamine-based 2-thiophenesulfonamide derivatives were prepared and their agonistic activity for the β-adrenergic receptors (ARs) was evaluated. Compound 54, containing 7-methanesulfonyloxy tryptamine, was found to be a highly potent β3-AR agonist (EC50 = 0.21 nM, IA = 97%) with excellent selectivity for the β3-AR over the β1- and β2-ARs (210- and 86-fold, respectively).
Keywords :
b3-Adrenergic receptor , agonist , fax: +816 63376010 , e-mail: kazuhiro-mizuno@dainippon-pharm.co.jp , Tryptamine.* Corresponding author. Tel.: +816 6337 5904
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
