Novel glutamic acid derived cholecystokinin receptor ligands
| Autor: | Victor J. Lotti, R. S. L. Chang, Roger M. Freidinger, Willie L. Whitter, M. K. Holloway, N. P. Gould |
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| Rok vydání: | 1990 |
| Předmět: |
Models
Molecular Chemical Phenomena Stereochemistry Guinea Pigs Molecular Conformation Peptide hormone Ligands digestive system Cholecystokinin receptor chemistry.chemical_compound Structure-Activity Relationship Glutamates Amide Drug Discovery Computer Graphics Animals Pancreas Cholecystokinin Gastrin Chemistry Chemistry Physical Ligand binding assay digestive oral and skin physiology Brain Glutamic acid Rats Biochemistry Lorglumide Molecular Medicine Receptors Cholecystokinin hormones hormone substitutes and hormone antagonists |
| Zdroj: | Journal of medicinal chemistry. 33(2) |
| ISSN: | 0022-2623 |
| Popis: | Novel aryl amide analogues of glutamic acid dialkylamide have been synthesized to test for a possible structural analogy between glutamic acid and benzodiazepine CCK antagonists such as compounds 2 and 24 (lorglumide and MK-329, respectively). In support of the structural model, certain of these hybrid compounds are more potent in pancreas CCK radioligand binding assays than corresponding lorglumide-type reference compounds. Modifications previously found in the benzodiazepine antagonists to result in brain CCK/gastrin receptor selectivity were also incorporated to produce an aryl urea series of glutamic acid analogues. None of these compounds were brain CCK/gastrin selective; however, one was potent and selective in the pancreas binding assay. The model appears to be most useful in the design of selective ligands for the pancreas type CCK receptor. |
| Databáze: | OpenAIRE |
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