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Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist.
L-364,718 exhibited a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays. Expand
A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260.
In vivo and in vivo, oral administration of L-365,260 antagonized gastrin-stimulated acid secretion in mice, rats, rats and guinea pigs, and did not antagonize histamine- or carbachol-stimulation in mice. Expand
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.
- J. O'brien, Wei Lemaire, +9 authors D. Williams
- Biology, Medicine
- Molecular pharmacology
- 1 September 2003
Evidence that allosteric sites on GPCRs can respond to closely related ligands with a range of pharmacological activities from positive to negative modulation as well as to neutral competition of this modulation is provided. Expand
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
- B. Evans, K. Rittle, +7 authors R. Chang
- Chemistry, Medicine
- Journal of medicinal chemistry
- 1 December 1988
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery. Expand
HETEROGENEITY OF HISTAMINE Hi‐RECEPTORS: SPECIES VARIATIONS IN [3H]MEPYRAMINE BINDING OF BRAIN MEMBRANES
The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined. Expand
Characterization of the binding of [3H]L-365,260: a new potent and selective brain cholecystokinin (CCK-B) and gastrin receptor antagonist radioligand.
The data indicates that [3H]L-365,260 represents a new potent nonpeptide antagonist radioligand suitable for the study of brain CCK-B and gastrin receptors. Expand
Two distinct angiotensin II receptor binding sites in rat adrenal revealed by new selective nonpeptide ligands.
The nonpeptide angiotensin II antagonists Dup-89 and WL-19 displaced specific 125I-angiotensin II binding in rat whole adrenal in a clearly biphasic manner, indicating the presence of high… Expand
Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors.
Data indicate that [3H]-(+/-)-L-364,718 represents a new potent nonpeptide antagonist radioligand for the study of peripheral CCK receptors which may allow differentiation of agonist and antagonist interactions. Expand
Methods for Drug Discovery: Development of Potent, Selective, Orally Effective Cholecystokinin Antagonists.