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  • Title: Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.
    Author: McDonald IM, Austin C, Buck IM, Dunstone DJ, Gaffen J, Griffin E, Harper EA, Hull RA, Kalindjian SB, Linney ID, Low CM, Patel D, Pether MJ, Raynor M, Roberts SP, Shaxted ME, Spencer J, Steel KI, Sykes DA, Wright PT, Xun W.
    Journal: J Med Chem; 2007 Oct 04; 50(20):4789-92. PubMed ID: 17850061.
    Abstract:
    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.
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