Non-peptide oxytocin agonists.
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).
Pitt
Gary R W
GR
Ferring Research Ltd, Chilworth Science Park, Southampton SO16 7NP, UK.
Batt
Andrzej R
AR
Haigh
Robert M
RM
Penson
Andrew M
AM
Robson
Peter A
PA
Rooker
David P
DP
Tartar
André L
AL
Trim
Julie E
JE
Yea
Christopher M
CM
Roe
Michael B
MB
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
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