NK3R Inhibitor

[MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC₅₀ value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).

NK3R-IN-2 is an orally active NK3R inhibitor with an IC₅₀ of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC₅₀ = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions.

GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pK_i of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pK_i = 5.2) and NK2 (pK_i = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.