Carbostyril oxytocin receptor antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514802, 514935, A61K 3147

Patent

active

053569040

ABSTRACT:
A method of inhibiting oxytocin from acting at its receptor site by administering oxytocin receptor antagonist compounds of the formula ##STR1## wherein X is oxygen or sulfur; Y is hydrogen or lower alkyl; R.sup.A is ##STR2##

REFERENCES:
patent: 5095003 (1992-03-01), Goetz et al.
Ogawa et al. 114 CA:81619f 1990.
The Pharmacological Basis of Therapeutics 7th Ed. Goodman & Gilmans Eds., The Macmillan Publ. Co. N.Y. 1987.
Life Sciences, vol. 50, pp. 1953-1958, Pergamon Press, (1992) By D. J. Pettibone, et al., entitled Radioligand BInding Studies Reveal Marked Species Differences in the Vasopressin V.sub.1 Receptor of Rat, Rhesus and Human Tissues.
Science, vol. 252, pp. 572-574 (Apr. 26, 1991) by Y. Yamamura, et al., entitled OPC-21268, An Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist.
Biochemical & Biophysical Research Communications, vol. 178, No. 2, pp. 707-712 (Jul. 31, 1991) by K. Okada, et al., entitled Effect of a New V.sub.1 Antagonist (OPC-21268) on Vascular Action of Vasopressin in Cultured Rat Vascular Smooth Muscle Cells.
Hypertension, vol. 18 (3), p. 383 (1991) by Y. Uehara, et al., entitled Alterations in Receptor-Mediated Activation of Phospholipase A.sub.2 in Dahl Salt-Sensitive Rats.

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