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).
MeSH terms
-
Angiotensin Receptor Antagonists
-
Animals
-
Antidiuretic Hormone Receptor Antagonists
-
Benzazepines / chemistry*
-
Benzazepines / metabolism
-
CHO Cells
-
Cell Line
-
Cricetinae
-
Dose-Response Relationship, Drug
-
Humans
-
Oxytocin / agonists*
-
Oxytocin / antagonists & inhibitors
-
Oxytocin / metabolism
-
Pyrrolidines / chemistry*
-
Pyrrolidines / metabolism
-
Receptors, Angiotensin / agonists
-
Receptors, Angiotensin / metabolism
-
Receptors, Oxytocin / agonists
-
Receptors, Oxytocin / antagonists & inhibitors
-
Receptors, Oxytocin / metabolism
-
Receptors, Vasopressin / agonists
-
Receptors, Vasopressin / metabolism
Substances
-
Angiotensin Receptor Antagonists
-
Antidiuretic Hormone Receptor Antagonists
-
Benzazepines
-
Nlrp6 protein, rat
-
OPC 51803
-
Pyrrolidines
-
Receptors, Angiotensin
-
Receptors, Oxytocin
-
Receptors, Vasopressin
-
Oxytocin