Effects of the non-peptide inhibitor OPC-21268 on oxytocin and vasopressin stimulation of rat and human myometrium

• Published in: European journal of pharmacology Vol. 281; no. 1; pp. 63 - 68
• Main Authors: Atke, Anders, Vilhardt, Hans, Hauzerova, Linda, Barth, Tom, Andersen, Lars Franch
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 25-07-1995; Elsevier
• Subjects: Anesthesia; Animals; Antidiuretic Hormone Receptor Antagonists; Biological and medical sciences; Cell Membrane - metabolism; Cell Membrane - ultrastructure; Dose-Response Relationship, Drug; Drug Interactions; Female; Genital system. Reproduction; Humans; In Vitro Techniques; Medical sciences; Myometrial receptor; Myometrium - drug effects; Myometrium - metabolism; Myometrium - ultrastructure; OPC-21268; Oxytocin; Oxytocin - antagonists & inhibitors; Oxytocin - pharmacology; Pharmacology. Drug treatments; Piperidines - metabolism; Piperidines - pharmacology; Pregnancy; Quinolones - metabolism; Quinolones - pharmacology; Rats; Receptors, Oxytocin - metabolism; Receptors, Vasopressin - metabolism; Sensitivity and Specificity; Stimulation, Chemical; Uterine Contraction - drug effects; Vasopressin; Vasopressin receptor antagonist; Vasopressins - antagonists & inhibitors; Vasopressins - pharmacology; Vasopressin receptor antagonist; Oxytocin; OPC-21268; Myometrial receptor; Vasopressin; Human; Myometrium; Rat; Peptide hormone; Rodentia; Smooth muscle; Neuropeptide; Muscle contraction; In vitro; Biological activity; Tocolytic; Pregnancy; Vertebrata; Mammalia; Uterus; Animal; Neurohypophyseal hormone; Peptidergic receptor; Antagonist
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/0014-2999(95)00225-A

OPC-21268 (1-[-1-[4-(3-acetylaminopropoxy)benzoyl]-piperidyl]-3,4-dihydro-2(1
H)-quinolinone), a non-peptide vasopressin V
1 receptor antagonist, inhibited oxytocin- and vasopressin-induced contractions of myometrial strips from rats and from full-term pregnant women. Administered intravenously in rats the drug also inhibited uterine contractions caused by infusion of oxytocin. When incubated with purified plasma membranes from rat or human myometrial tissue, OPC-21268 inhibited the specific receptor binding of tritiated oxytocin and vasopressin in a dose-dependent and reversible way.