Cholecystokinin antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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A01K 3155

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active

052062384

ABSTRACT:
Compounds of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecycstokinin (CCK) and have properties useful for treating panic disorder and for directly inducing anlagesia.

REFERENCES:
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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 Benzodiazepine 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. Morhpine Induced Analgesia in the 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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