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Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties. | LitMetric

Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Biochemistry and Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.

Published: February 2001

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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http://dx.doi.org/10.1016/s0960-894x(00)00669-7DOI Listing

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