title: Non-peptide oxytocin agonists.
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).
authors.affiliation: Ferring Research Ltd, Chilworth Science Park, Southampton SO16 7NP, UK.
authors.forename: Gary R W
authors.initials: GR
authors.lastname: Pitt
authors.forename: Andrzej R
authors.initials: AR
authors.lastname: Batt
authors.forename: Robert M
authors.initials: RM
authors.lastname: Haigh
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Penson
authors.forename: Peter A
authors.initials: PA
authors.lastname: Robson
authors.forename: David P
authors.initials: DP
authors.lastname: Rooker
authors.forename: André L
authors.initials: AL
authors.lastname: Tartar
authors.forename: Julie E
authors.initials: JE
authors.lastname: Trim
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Yea
authors.forename: Michael B
authors.initials: MB
authors.lastname: Roe
mesh_terms: D057911:Angiotensin Receptor Antagonists; D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines / Q000737:chemistry* / Q000378:metabolism; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010121:Oxytocin / Q000819:agonists* / Q000037:antagonists & inhibitors / Q000378:metabolism; D011759:Pyrrolidines / Q000737:chemistry* / Q000378:metabolism; D011945:Receptors, Angiotensin / Q000819:agonists / Q000378:metabolism; D018045:Receptors, Oxytocin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D017483:Receptors, Vasopressin / Q000819:agonists / Q000378:metabolism
chemical_list: D057911:Angiotensin Receptor Antagonists; D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines; C456360:Nlrp6 protein, rat; C409942:OPC 51803; D011759:Pyrrolidines; D011945:Receptors, Angiotensin; D018045:Receptors, Oxytocin; D017483:Receptors, Vasopressin; D010121:Oxytocin