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Bioorg Med Chem Lett ; 14(17): 4585-9, 2004 Sep 06.
Article in English | MEDLINE | ID: mdl-15357997

ABSTRACT

A library of compounds targeted to the vasopressin/oxytocin family of receptors was screened for activity at a cloned human oxytocin receptor using a reporter gene assay. Potency and selectivity were optimised to afford compound 39, EC50 = 33 nM. This series of compounds represents the first disclosed, non-peptide, low molecular weight agonists of the hormone oxytocin (OT).


Subject(s)
Benzazepines/chemistry , Oxytocin/agonists , Pyrrolidines/chemistry , Angiotensin Receptor Antagonists , Animals , Antidiuretic Hormone Receptor Antagonists , Benzazepines/metabolism , CHO Cells , Cell Line , Cricetinae , Dose-Response Relationship, Drug , Humans , Oxytocin/antagonists & inhibitors , Oxytocin/metabolism , Pyrrolidines/metabolism , Receptors, Angiotensin/agonists , Receptors, Angiotensin/metabolism , Receptors, Oxytocin/agonists , Receptors, Oxytocin/antagonists & inhibitors , Receptors, Oxytocin/metabolism , Receptors, Vasopressin/agonists , Receptors, Vasopressin/metabolism
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