916508-97-9Relevant academic research and scientific papers
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists
McDonald, Iain M.,Austin, Carol,Buck, Ildiko M.,Dunstone, David J.,Gaffen, John,Griffin, Eric,Harper, Elaine A.,Hull, Robert A. D.,Kalindjian, S. Barret,Linney, Ian D.,Low, Caroline M. R.,Patel, Dipa,Pether, Michael J.,Raynor, Michelle,Roberts, Sonia P.,Shaxted, Mark E.,Spencer, John,Steel, Katherine I. M.,Sykes, David A.,Wright, Paul T.,Xun, Wei
, p. 4789 - 4792 (2007)
A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.
