Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties |
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| Authors: | 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 |
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| Institution: | Department of Medicinal Chemistry, Biochemistry and Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA. |
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| Abstract: | 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. |
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