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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Pharmacology of CCKRs and SAR Studies of Peptidic Analog Ligands

Author(s): Florence Noble

Volume 7 , Issue 12 , 2007

Page: [1173 - 1179] Pages: 7

DOI: 10.2174/156802607780960447

Price: $65


Cholecystokinin (CCK) is a peptide originally discovered in the gastrointestinal tract but also found in high density in the mammalian brain. The C-terminal sulphated octapeptide fragment of cholecystokinin (CCK8) constitutes one of the major neuropeptides in the brain. CCK8, interacting with nanomolar affinities with two different receptors designated CCK1 and CCK2, has been shown to be involved in numerous physiological functions and is involved in the modulation/control of multiple central functions. In particular, CCK is involved in the neurobiology of anxiety, depression, psychosis, cognition, nociception and feeding behavior. The functional role of CCK has been facilitated thanks to the development of potent and selective CCK receptor antagonists and agonists. In this review, the strategies followed to design peptidic analog ligands will be reported, as the pharmacology of CCK receptors.

Keywords: CCK2 Antagonists, antinociceptive effects, opioids, Structure-affinity relationships, CCK2 receptor

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