Novel, Achiral 1,3,4-benzotriazepine Analogues of 1,4-benzodiazepine-based Cck(2) Antagonists That Display High Selectivity over Cck(1) Receptors.
From: James Black Foundation, 68 Half Moon Lane, Dulwich, London, SE24 9JE, UK. iain.mcdonald@kcl.ac.uk
Journal of medicinal chemistry
- Publish Date: Apr 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 7
- Pages: 2253-61
- Medium: Print
- Language: English
- Citation (JAMA): McDonald Iain M, Austin Carol, Buck Ildiko M, et al. Novel, Achiral 1,3,4-benzotriazepine Analogues of 1,4-benzodiazepine-based Cck(2) Antagonists That Display High Selectivity over Cck(1) Receptors.. J. Med. Chem. Apr 2006;49:2253-61
Abstract
A series of 1,3,4-benzotriazepine-based CCK(2) antagonists have been devised by consideration of the structural features that govern CCK receptor affinity and the receptor subtype selectivity of 1,4-benzodiazepine-based CCK(2) antagonists. In contrast to the latter compounds, these novel 1,3,4-benzotriazepines are achiral, yet they display similar affinity for CCK(2) receptors to the earlier molecules and are highly selective over CCK(1) receptors.
Mesh Headings (Keywords): Animals, Benzazepines, Benzodiazepines, Cell Line, Cricetinae, Cricetulus, Crystallography, X-Ray, Humans, Mice, Molecular Structure, Radioligand Assay, Rats, Receptor, Cholecystokinin A, Receptor, Cholecystokinin B, Stereoisomerism, Structure-Activity Relationship
Check for Full Text / PubMed Unique Identifier (PMID): 16570921
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