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Synonyms: C4.6,S1-cyclo[N-(3-sulfanylpropanoyl)-D-tryptophyl-L-isoleucyl-L-alloisoleucyl-L-asparaginyl-L-2-aminobutanoyl-N-methyl-L-ornithinol] | FE 200 440  | FE-200440
Compound class: Peptide or derivative
Comment: Barusiban (FE 200440) is an oxytocin receptor antagonist [1-2,5]. It was developed by Ferring Pharmaceuticals as a tocolytic agent, to counteract oxytocin-induced myometrial contractions . Chemically it is a synthetic cyclic hexapeptide containing five unnatural amino acids and only one D-amino acid.
|Barusiban has almost no effect on vasopressin-induced contractions of isolated term-pregnant human myometrium. It inhibits oxytocin-induced human myometrial contractions in vitro with a pA2 of 8.3. In contrast the pA2 for atosiban in the same experiment is 10.6, but atosiban also inhibits vasopressin-induced contractility.|