L-368,899 is a drug used in scientific research which acts as a selective
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, ri ...
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 good 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.
Unlike related drugs such as the peripherally selective
L-371,257
L-371,257 is a compound used in scientific research which acts as a selective antagonist of the oxytocin receptor with over 800x selectivity over the related vasopressin receptors. It was one of the first non-peptide oxytocin antagonists develope ...
, the oral bioavailabity is high and the brain penetration of L-368,899 is rapid, with selective accumulation in areas of the
limbic system
The limbic system, also known as the paleomammalian cortex, is a set of brain structures located on both sides of the thalamus, immediately beneath the medial temporal lobe of the cerebrum primarily in the forebrain.Schacter, Daniel L. 2012. ''P ...
. This makes it a useful tool for investigating the centrally mediated roles of oxytocin, such as in social behaviour and
pair bond
In biology, a pair bond is the strong affinity that develops in some species between a mating pair, often leading to the production and rearing of offspring and potentially a lifelong bond. Pair-bonding is a term coined in the 1940s that is freque ...
ing, and studies in primates have shown L-368,899 to reduce a number of behaviours such as food sharing, sexual activity and caring for infants, demonstrating the importance of oxytocinergic signalling in mediating these important social behaviours.
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 ...
*
Barusiban
Barusiban (International Nonproprietary Name, INN) (code name FE-200440) is a non-peptide drug which is among the most potent and selective oxytocin receptor receptor antagonist, antagonists known. It was clinical trial, trialed by Ferring Pharma ...
*
Epelsiban
Epelsiban ( INN, USAN, code name GSK-557,296-B) is an orally bioavailable drug which acts as a selective and potent oxytocin receptor antagonist ( Ki = 0.13 nM). It was initially developed by GlaxoSmithKline (GSK) for the treatment of premature ...
*
L-371,257
L-371,257 is a compound used in scientific research which acts as a selective antagonist of the oxytocin receptor with over 800x selectivity over the related vasopressin receptors. It was one of the first non-peptide oxytocin antagonists develope ...
*
Retosiban
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 ...
References
{{Oxytocin and vasopressin receptor modulators
Oxytocin receptor antagonists
Phenylpiperazines
Tocolytics
2-Tolyl compounds