Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties

…, JH Weng, A Dorville, I McCort, B Ducos…

Index: Blommaert, Armand G.S.; Weng Jian-Hui; Dorville, Agnes; McCort, Isabelle; Ducos, Bertrand; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2868 - 2877

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Citation Number: 52

Abstract

Antagonists of cholecystokinin-B (CCK-B) receptors have been shown to alleviate CC&- induced panic attacks in humans and to potentiate opioid effects in animals. The clinical use of these compounds is critically dependent on their ability to cross the blood-brain barrier. In order to improve this property, new, peptoid-derived CCK-B antagonists, endowed with high affinity, selectivity, and increased lipophilicity have been developed. The affinity and ...