barusiban

Names

[ Name ]:
barusiban

[Synonym ]:
FE200 440
Barusiban [INN]
UNII-UX33I93GLS
Barusiban
C4.6,S1-Cyclo(N-(3-sulfanylpropanoyl)-D-tryptophyl-L-isoleucyl-L-alloisoleucyl-L-asparaginyl-L-2-aminobutanoyl-N-methyl-L-ornithinol)

Biological Activity

[Description]:

Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research[1][2][3].

[Related Catalog]:

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor

[In Vitro]

Barusiban shows affinity for oxytocin receptor (Ki=0.8 nM) in COS cells expressed with oxytocin receptor[3].

[In Vivo]

Barusiban (intravenous injection; 50 or 150 μg/kg; once) treatment shows inhibition on OT-induced contractions[2]. Animal Model: Pregnant cynomolgus monkeys injected with oxytocin (OT)[2] Dosage: 50 or 150 μg/kg Administration: Intravenous injection; 50 or 150 μg/kg; once Result: Reduced uterine contractions to baseline levels effectively. Reduced intrauterine pressure (IUP) from 6-7.5 kmm Hg•h to approximately 1 kmm Hg•h.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₀H₆₃N₉O₈S

[ Molecular Weight ]:
830.04900

[ Exact Mass ]:
829.45200

[ PSA ]:
314.68000

[ LogP ]:
3.41670

Related Compounds

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