A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260
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Biological behavior of 1, 4-benzodiazepines and 1, 4-benzothiazepines
2022, Benzodiazepine-Based Drug DiscoveryDesign and synthesis of novel 1,4-benzodiazepine surrogates as potential CCKA and CCKB antagonists via palladium-catalyzed three-component cascade reactions
2018, TetrahedronCitation Excerpt :Using identical reaction conditions than those described before, substituted and unsubstituted allenes 7 were allowed to react with aryl halides 6 and heterocycle 9a, in the presence of Pd2(dba)3 (10 mol%) and PPh3 (20 mol%) in DMF at 80 °C for 48 h. Functionalized compounds 10a-d were obtained in 65–92% yield in one pot cascade reaction (Scheme 3). X-Ray diffraction analysis of structure 10a28 also confirmed the skeleton drawn in Scheme 3. A third series of benzodiazepine-2-one analogues were prepared from 5 or 9 but employing carbon monoxide instead of allenes as relay species in the cascade processes.
The role of cholecystokinin receptors in the short-term control of food intake
2013, Progress in Molecular Biology and Translational ScienceNeuropeptide regulation of fear and anxiety: Implications of cholecystokinin, endogenous opioids, and neuropeptide Y
2012, Physiology and BehaviorCitation Excerpt :Both receptors belong to the super family of G-protein coupled receptors, and couple to Gq. CCK-A has a high affinity for sulphated CCK-8 (CCK-8S), where CCK-B is equally selective for CCK-8S, non-sulphated CCK-8 (CCK-8 N), CCK-4, and CCK-5 [37–39]. Initial behavioral studies showed impairment of acquisition of active avoidance with IP administration of sulphated and non-sulphated CCK-8.
Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor
2012, Journal of Biological ChemistrySynthesis and structure-activity relationship of new 1,5-dialkyl-1,5- benzodiazepines as cholecystokinin-2 receptor antagonists
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :The CCK1 receptor subtypes are involved both in the control of the gall bladder and in the digestive enzyme secretion, while the CCK2 subtypes are mainly responsible for neurotransmission and neuromodulation. In particular, during the last years, it has been demonstrated that CCK2 antagonists are targets for anxiety and panic.2–7 Many different classes of compounds have been reported as CCK2 antagonists8: 1,4-benzodiazepines3 and 1,3,4-benzotriazepines9, dipeptoids10, quinazolines11, pyrazolidinones12, quinazolinones.13