The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.
Liddle
John
J
Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. john.2.liddle@gsk.com
Allen
Michael J
MJ
Borthwick
Alan D
AD
Brooks
David P
DP
Davies
David E
DE
Edwards
Richard M
RM
Exall
Anne M
AM
Hamlett
Chris
C
Irving
Wendy R
WR
Mason
Andrew M
AM
McCafferty
Gerald P
GP
Nerozzi
Fabrizio
F
Peace
Simon
S
Philp
Joanne
J
Pollard
Derek
D
Pullen
Mark A
MA
Shabbir
Shaila S
SS
Sollis
Steve L
SL
Westfall
Timothy D
TD
Woollard
Pat M
PM
Wu
Charlene
C
Hickey
Deirdre M B
DM
D000818:Animals; D005260:Female; D006801:Humans; D007700:Kinetics; D010121:Oxytocin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010879:Piperazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018045:Receptors, Oxytocin / Q000378:metabolism; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
C522194:GSK221149A; D010879:Piperazines; D018045:Receptors, Oxytocin; D010121:Oxytocin