L-371,257
Encyclopedia
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 receptor
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.
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
Vasopressin receptor
A vasopressin receptor is a cell surface receptor which binds vasopressin. The three types of vasopressin receptor are members of the A6 subfamily of G-protein coupled receptors.-Subtypes:Humans express three subtypes: 1A, 1B and 2-Function:...
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
Blood-brain barrier
The blood–brain barrier is a separation of circulating blood and the brain extracellular fluid in the central nervous system . It occurs along all capillaries and consists of tight junctions around the capillaries that do not exist in normal circulation. Endothelial cells restrict the diffusion...
which gives it good peripheral selectivity with few central side effects. Potential applications are likely to be in the treatment of premature labour.