Brockunier L L, Candelore M R, Cascieri M A, Liu Y, Tota L, Wyvratt M J, Fisher M H, Weber A E, Parmee E R
Department of Medicinal Chemistry, Biochemistry and Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2001 Feb 12;11(3):379-82. doi: 10.1016/s0960-894x(00)00669-7.
Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylenediamine moieties were examined as human beta3 adrenergic receptor (AR) agonists. Notably, indoline derivatives 6a and 11 were potent beta3 AR agonists (beta3 EC50 = 13 and 19 nM, respectively), which showed good selectivity over binding to and minimal activation of the beta1 and beta2 ARs.
含有氰基胍或硝基乙二胺部分的吡啶乙醇胺衍生物作为人β3肾上腺素能受体（AR）激动剂进行了研究。值得注意的是，吲哚啉衍生物6a和11是强效β3 AR激动剂（β3 EC50分别为13和19 nM），它们对β1和β2 ARs的结合表现出良好的选择性且激活作用最小。
