1387566-98-4Relevant academic research and scientific papers
Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: Clinical compound TD-2749
Long, Daniel D.,Armstrong, Scott R.,Beattie, David T.,Choi, Seok-Ki,Fatheree, Paul R.,Gendron, Roland A.L.,Goldblum, Adam A.,Humphrey, Patrick P.,Marquess, Daniel G.,Shaw, Jeng-Pyng,Smith, Jacqueline A.M.,Derek Turner,Vickery, Ross G.
, p. 4849 - 4853 (2012)
Further application of our multivalent approach to drug discovery directed to 5-HT4 receptor agonists is described. Optimization of the linker and secondary binding amine in the indazole-tropane primary binding group series, for binding affinity and functional potency at the 5-HT4 receptor, selectivity over the 5-HT3 receptor, oral pharmacokinetics, and in vivo efficacy in models of GI motility, resulted in the identification of clinical compound TD-2749.
