NK1 Receptor Agonists Small Molecules and Peptides

The neurokinin 1 (NK₁) receptor is a member of the tachykinin family of G-protein-coupled receptors which also includes NK₂ and NK₃ receptors. The NK₁ receptor is localized in high concentrations in the CNS (particularly the striatum, amygdala and some hypothalamic and thalamic nuclei) and peripheral tissues.

NK₁ receptors are thought to mediate central stress reactions, mood control, excitatory neurotransmission, immune modulation and airway and lung function. The receptor displays greater potency for the endogenous agonist substance P than Neurokinin A and Neurokinin B (SP > NKA > NKB). The human gene encoding the NK₁ receptor has been localized on chromosome 2 (2p13.1-p12).