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1. Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: Tuning of receptor selectivity and in vivo efficacy

Author

Pippel, Marna, Boyce, Kristen, Venkatesan, Hariharan, Phuong, Victor K., Yan, Wen, Barrett, Terrance D., Lagaud, Guy, Li, Lina, Morton, Magda F., Prendergast, Clodagh, Wu, Xiaodong, Shankley, Nigel P., and Rabinowitz, Michael H.

Subjects
*SULFONAMIDES, *CHOLECYSTOKININ, *HORMONE antagonists, *OXAZOLES, *PHARMACOKINETICS, *LABORATORY rats, *GASTRIC acid, *AMYLASES, *DRUG efficacy, *THERAPEUTICS
Abstract

Abstract: In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics properties and in vivo efficacy in rat models of gastric acid and pancreatic amylase secretion. [Copyright &y& Elsevier]

Published
2009
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