Cholecystokinin antagonists

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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514221, A61K 3155, C07D24324

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active

052200175

ABSTRACT:
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

REFERENCES:
patent: 4820834 (1991-04-01), Evans et al.
Bradwejn, et al., Enhanced Sensitivity to Cholecystokinin Tetrapeptide in Panic Disorder, Soc. Neurosci. Abstr. 14(1), p. 291, (1988).
de Montigny, Cholecystokinin Tetrapeptide Induces Panic Attacks in Healthy Volunteers, Soc. Neurosci. Abstr. 14(1), p. 291, (1988).
Bradwejn, et al., Benzodiazepines Antagonize Cholecystokinin-Induced Activation of Rat Hippocampal, Neurones, Nature 312, p. 22, (1984).
de Montigny, Cholecystokinin Tetrapeptide Induces Panic-like Attacks in Healthy Volunteers, Arch. Gen Psychiatry, 46, pp. 511-517, (1989).
Dourish, et al., Enhancement of Morphine Analgesia and Prevention of Morphine Tolerance in the Rat by the Cholecystokinin Antagonist L-364, 718 Pharm. 147, pp. 469-472, (1988).
Bouthillier, et al., Long-term Benzodiazephine Treatment Reduces Neuronal Responsiveness to Cholecystokinin: an Electrophysiological Study in the Rat, Eur. Jour. Pharm. 151, No. 1, pp. 135-138, (1988).
O'Neill et al. Morphine Induced Analgesia int he Rat Paw Pressure Test is Blocked by CCK and Enhanced by the CCK Antagonist MK-329, Neuropharmacology 28, No. 3, pp. 243-247 (1989).
Chang, et al., Biochemical and Pharmacological Characterization of an Extremely Potent and Selective Nonpeptide Cholecystokinin Antagonist, Proc. Natl. Acad. Sci., 83, pp. 4923-4926 (1986).
Bock, et al., Benzodiazepine Gastrin and Brain Cholecystokinin Receptor Ligands: L-365, 260, Journal of Medicinal Chemistry, 32, No. 1, pp. 13-16 (1989).

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