nk-3r

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM against human NK3R. It can penetrate the blood-brain barrier and exhibits excellent NK3R binding affinity in CHO-K1 cells (IC50= 87.31 nM). NK3R-IN-2 effectively suppresses luteinizing hormone (LH) levels and is applicable for research on hormone-related diseases.

NK3R-IN-1 (compound 16x), an orally active imidazolepiperazine derivative, functions as a Neurokinin Receptor NK3R inhibitor and has been demonstrated to reduce blood luteinizing hormone concentrations in an ovariectomy (OVX) model [1].

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. It holds potential for research in the treatment of nausea and vomiting related to cancer or postoperative conditions.