NK3 Receptor Antagonists Small Molecules and Peptides

The neurokinin 3 (NK₃) receptor is a member of the tachykinin family of G-protein-coupled receptors which also includes NK₁ and NK₂ receptors. The NK₃ receptor is predominantly expressed in the CNS (hippocampus, hypothalamus, substantia nigra, dorsal horn of the spinal cord) with limited expression in the periphery.

NK₃ receptors are thought to mediate afferent neuron transmission and intestinal motility and secretion. The receptor displays greater potency for the endogenous agonist neurokinin B than neurokinin A and substance P (NKB > NKA > SP). The human gene encoding the NK₃ receptor has been localized on chromosome 4 (4q25).