retosiban
Sign in to saveAlso known as GSK-221,149-A
Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour. Retosiban has high affinity for the oxytocin receptor (Ki = 0.65 nM) and has greater than 1400-fold selectivity over the related vasopressin receptors
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 494.25292018799996
Show 4 more facts
- Commons category
- Retosiban
- isomeric SMILES
- CC[C@H](C)[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c2coc(n2)C)C(=O)N3CCOCC3)C4Cc5ccccc5C4
- chemical formula
- C₂₇H₃₄N₄O₅
- canonical SMILES
- CCC(C)C1C(=O)NC(C2Cc3ccccc3C2)C(=O)N1C(C(=O)N1CCOCC1)c1coc(C)n1
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Encyclopedic overview
7 sectionsContents
- Mechanism of action
- Pharmacology
- Pharmacokinetics
- Physical and chemical properties
- Synthesis
- See also
- References
Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour. Retosiban has high affinity for the oxytocin receptor (Ki = 0.65 nM) and has greater than 1400-fold selectivity over the related vasopressin receptors
==Mechanism of action== Retosiban is a competitive oxytocin receptor antagonist which blocks the oxytocin-mediated contraction of the uterine smooth muscle in the female uterus that occurs during the initiation of preterm labour. This has been used to prevent preterm labour and premature birth.
Excerpted from Wikipedia’s “retosiban” article, available under the CC BY-SA 4.0 licence.