L-371,257 is a compound used in scientific research which acts as a selective
antagonist of the
oxytocin receptor
The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. In humans, the oxytocin receptor is encoded by the ''OXTR'' gene which has been localized to human chromosome 3p25. ...
with over 800x selectivity over the related
vasopressin receptor
The actions of vasopressin are mediated by stimulation of tissue-specific G protein-coupled receptors (GPCRs) called vasopressin receptors that are classified into the V1 (V1A), V2, and V3 (V1B) receptor subtypes. These three subtypes diffe ...
s. It was one of the first non-peptide oxytocin antagonists developed, and has good oral bioavailability, but poor penetration of the
blood–brain barrier, which gives it good peripheral selectivity with few central side effects. Potential applications are likely to be in the treatment of premature labour.
See also
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Atosiban
Atosiban, sold under the brand name Tractocile among others, is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. It was developed by Ferri ...
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Barusiban
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Epelsiban
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L-368,899
L-368,899 is a drug used in scientific research which acts as a selective antagonist of the oxytocin receptor, with good selectivity over the related vasopressin receptors. Unlike related drugs such as the peripherally selective L-371,257, the ora ...
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Retosiban
References
{{Oxytocin and vasopressin receptor modulators
Tocolytics
Oxytocin receptor antagonists
Peripherally selective drugs