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  • Title: Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
    Author: Pippel M, Allison BD, Phuong VK, Li L, Morton MF, Prendergast C, Wu X, Shankley NP, Rabinowitz MH.
    Journal: Bioorg Med Chem Lett; 2009 Nov 15; 19(22):6373-5. PubMed ID: 19811913.
    Abstract:
    A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold.
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