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Retosiban information


Retosiban
Clinical data
Other namesGSK-221149-A
ATC code
  • None
Legal status
Legal status
  • In general: non-regulated
Identifiers
IUPAC name
  • (3R,6R)-6-[(2S)-butan-2-yl]-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2-methyl-1,3-oxazol-4-yl)-2-(morpholin-4-yl)-2-oxoethyl]piperazine-2,5-dione
CAS Number
  • 820957-38-8
PubChem CID
  • 11340891
ChemSpider
  • 9515833
UNII
  • GIE06H28OX
KEGG
  • D08986
CompTox Dashboard (EPA)
  • DTXSID00231559 Edit this at Wikidata
Chemical and physical data
FormulaC27H34N4O5
Molar mass494.592 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CC[C@H](C)[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](C2=COC(=N2)C)C(=O)N3CCOCC3)C4CC5=CC=CC=C5C4
InChI
  • InChI=1S/C27H34N4O5/c1-4-16(2)23-25(32)29-22(20-13-18-7-5-6-8-19(18)14-20)26(33)31(23)24(21-15-36-17(3)28-21)27(34)30-9-11-35-12-10-30/h5-8,15-16,20,22-24H,4,9-14H2,1-3H3,(H,29,32)/t16-,22+,23+,24+/m0/s1
  • Key:PLVGDGRBPMVYPB-FDUHJNRSSA-N

Retosiban also known as GSK-221,149-A[1][2] is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour.[3][4] Retosiban has high affinity for the oxytocin receptor (Ki = 0.65 nM) and has greater than 1400-fold selectivity[5] over the related vasopressin receptors

  1. ^ Liddle J, Allen MJ, Borthwick AD, Brooks DP, Davies DE, Edwards RM, et al. (January 2008). "The discovery of GSK221149A: a potent and selective oxytocin antagonist". Bioorganic & Medicinal Chemistry Letters. 18 (1): 90–4. doi:10.1016/j.bmcl.2007.11.008. PMID 18032036.
  2. ^ Borthwick AD, Liddle J (January 2013). "Retosiban and Epelsiban: Potent and Selective Orally available Oxytocin Antagonists". In Domling A (ed.). Methods and Principles in Medicinal Chemistry: Protein-Protein Interactions in Drug Discovery. Weinheim: Wiley-VCH. pp. 225–256. doi:10.1002/9783527648207.ch10. ISBN 978-3-527-33107-9.
  3. ^ USAN Council (2007). "Statement on a Nonproprietary Name Adopted by the USAN Council" (PDF).
  4. ^ Borthwick AD, Liddle J (July 2011). "The Design of Orally Bioavailable 2,5-Diketopiperazine Oxytocin Antagonists: From Concept to Clinical Candidate for Premature Labour". Medicinal Research Reviews. 31 (4): 576–604. doi:10.1002/med.20193. PMID 20027670. S2CID 22514154.
  5. ^ McCafferty GP, Pullen MA, Wu C, Edwards RM, Allen MJ, Woollard PM, Borthwick AD, Liddle J, Hickey DM, Brooks DP, Westfall TD (2007). "Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. 293 (1): R299–305. doi:10.1152/ajpregu.00057.2007. PMID 17395790.

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Retosiban

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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...

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Dipeptide

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BioTopics. Retrieved 28 July 2014. Borthwick AD, Liddle J (January 2013). "Retosiban and Epelsiban: Potent and Selective Orally available Oxytocin Antagonists"...

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Vasopressin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Diketopiperazine

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hdl:10033/243651. PMID 22709011. Borthwick AD, Liddle J (January 2013). "Retosiban and Epelsiban: Potent and Selective Orally available Oxytocin Antagonists"...

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Desmopressin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Oxytocin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Atosiban

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Oxytocin receptor

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blood brain barrier penetration, few central effects) L-372,662 Nolasiban Retosiban (GSK-221,149) SSR-126,768 WAY-162,720 – centrally active following peripheral...

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Lithium carbonate

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Oxytocin receptor agonist

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Carbetocin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Terlipressin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Tolvaptan

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Vasopressin receptor antagonist

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Vasopressin receptor

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Demeclocycline

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Vasopressin receptor 2

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Conivaptan

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Vasotocin

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Uterotonic

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Neurophysin I

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Cligosiban Epelsiban Erlosiban IX-01 L-368,899 L-371,257 L-372,662 Nolasiban Retosiban SSR-126768 WAY-162720 Catabolism inhibitors: Amastatin Bestatin (ubenimex)...

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Barusiban

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and was not pursued any further. Atosiban Epelsiban L-368,899 L-371,257 Retosiban Landgraf R, Neumann ID (10 September 2008). Advances in Vasopressin and...

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