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Article

New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R).

Journal of medicinal chemistry - 25 Aug 2011

Pavan Michela V, Lassiani Lucia, Berti Federico, Stefancich Giorgio, Ciogli Alessia, Gasparrini Francesco, Mennuni Laura, Ferrari Flora, Escrieut Chantal, Marco Esther, Makovec Francesco, Fourmy Daniel, Varnavas Antonio

Abstract excerpt

The anthranilic acid diamides represent the most recent class of nonpeptide CCK(1) receptor (CCK(1)-R) antagonists. Herein we describe the second phase of the anthranilic acid C-terminal optimization using nonproteinogenic amino acids containing a phenyl ring in their side chain. The Homo-Phe derivative 2 (VL-0797) enhanced 12-fold the affinity for the rat CCK(1)-R affinity and 15-fold for the human CCK(1)-R...

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PMID: 21728335
DOI: 10.1021/jm200438b

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CCK

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