Retosiban, GSK221149A
820957-38-8
MW 494.5827, MF C27 H34 N4 O5
Oxytocin antagonist
Threatened pre-term labour
PHASE 3 GSK
UNII-GIE06H28OX, GSK 221149A, 820957-38-8,
(3R,6R)-6-((S)-sec-butyl)-3-(2,3-dihydro-1H-inden-2-yl)-1-((R)-1-(2-methyloxazol-4-yl)-2-morpholino-2-oxoethyl)piperazine-2,5-dione
3(R)-(2,3-Dihydro-1H-inden-2-yl)-1-[1(R)-(2-methyloxazol-4-yl)-2-(4-morpholinyl)-2-oxoethyl]-6(R)-[1(S)-methylpropyl]piperazine-2,5-dione
(3R.6R)-3-(2,3-dihvdro-1 H-inden-2-v0-1 -( R)-1 -(2-methyl-1 ,3-oxazol-4- yl)-2-(4-morpholinyl)-2-oxoethyll-6-r(1S -1-methylpropyn-2.5- piperazinedione
2,5-Piperazinedione, 3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2-methyl-4-oxazolyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-, (3R,6R)-
Morpholine, 4-[(2R)-[(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-6-[(1S)-1-methylpropyl]-2,5-dioxo-1-piperazinyl](2-methyl-4-oxazolyl)acetyl]-
Retosiban (GSK-221,149-A)[1][2] is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptorantagonist with >1400-fold selectivity[3] over the related vasopressin receptors and is being developed by GlaxoSmithKline for the treatment of preterm labour.[4][5]
Retosibanis an oxytocin (OT) antagonist in phase III clinical trials at GlaxoSmithKline for the prevention of preterm labor. OT antagonism is widely known to inhibit spontaneous uterine contractions.
Retosiban is a diketopiperazine nonpeptide compound with high potency and selectivity for the OT receptor over vasopressin receptors.
This candidate has been shown to block oxytocin-induced…
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