CCKBselective

CCKBselective refers to compounds and ligands that preferentially bind to the cholecystokinin B receptor (CCK-B, also called CCK2). The term is used in pharmacology to indicate selectivity for CCK-B over the CCK-A (CCK1) receptor, or to denote ligands that produce a greater functional response at CCK-B receptors. CCK-B receptors are G protein-coupled receptors primarily expressed in the brain and stomach; endogenous ligands include cholecystokinin and gastrin.

In the brain, CCK-B receptors are found in regions such as the amygdala and hippocampus and are implicated in anxiety, fear conditioning, learning, and feeding behavior; in the gut, they regulate gastric acid secretion and enzyme release.

CCKBselective ligands include peptide and nonpeptide compounds used in preclinical research. Potent antagonists are commonly employed to probe receptor function and to test therapeutic hypotheses, while agonists can be used to elicit receptor-mediated responses. Well-known examples cited in the literature include the peptide antagonist L-365,260 and nonpeptide antagonists such as CI-988; however, the specificity and pharmacokinetics can vary across species.

Most CCK-B selective agents have been studied in animal models of anxiety and gastric function, and some have been evaluated in early-phase clinical studies for anxiety or peptic disorders, but no CCK-B selective drug has gained regulatory approval to date due to limited efficacy and safety concerns.

Currently, the term remains a descriptor in pharmacology and medicinal chemistry, guiding the development of receptor-selective probes and potential therapeutics.