102428-91-1Relevant academic research and scientific papers
Cholecystokinin antagonists for treating neurological disorders
-
, (2008/06/13)
Compounds of the formula: are disclosed which are antagonists of gastrin and cholecycstokinin (CCK) and have properties useful for treating panic disorder and for directly inducing anlagesia.
Cholecystokinin-A Receptor Ligands Based on the κ-Opioid Agonist Tifluadom
Bock, Mark G.,DiPardo, Robert M.,Evans, Ben E.,Rittle, Kenneth E.,Whitter, Willie L.,et al.
, p. 450 - 455 (2007/10/02)
Tifluadom, a k-opioid agonist and cholecystokinin-A (CCK-A) receptor antagonist, was utilized as a model to prepare a series of 2-(aminomethyl)- and 3-(aminomethyl)-1,4-benzodiazepines.These compounds were tested in vitro as inhibitors of the binding of CCK to rat pancreas and guinea pig brain receptors.All compounds with IC50's less than 100 μM proved to have greater affinity for the CCK-A receptor, with the most potent analogue, 6e, having an IC50 of 0.16 μM.The benzodiazepines described in this study are simultaneously CCK-A and opioid receptor ligands.The ramification of this dichotomy on current concepts of peptide horm one action are discussed.These results further demonstrate the versatility of the benzodiazepine core structure for designing nonpeptide ligands for peptide receptors and the ability to fine-tune the receptor interactions of these benzodiazepines by appropiate structure modifications.
2-substituted-aminomethyl-1,4-benzodiazepines
-
, (2008/06/13)
Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antago
