Netupitant

Netupitant is an insurmountable antagonist of the neurokinin-1 (NK₁) receptor (K_i = 0.95 nM in CHO cells expressing the human recombinant receptor).¹ It is selective for human NK₁ over human NK₂ and NK₃ and rat NK₁ (K_is = >1,500 nM) and over 50 G protein-coupled receptors, monoamine transporters, and ion channels when used in the nanomolar range.² Netupitant decreases the maximal response to substance P-induced contractions in isolated guinea pig ileum with long-lasting effects. It also dose-dependently inhibits the substance P-induced scratching, biting, and licking response in mice when used at doses ranging from 1-10 mg/kg and decreases NK agonist-induced foot tapping in gerbils (ID₅₀s = 1.5 mg/kg, i.p., or 0.5 mg/kg, oral). Formulations containing netupitant have been used in the treatment of chemotherapy-induced nausea and vomiting.

WARNING This product is not for human or veterinary use.

1. Hoffmann, T., Bös, M., Stadler, H., et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg. Med. Chem. Lett. 16(5), 1362-1365 (2006).

2. Rizzi, A., Campi, B., Camarda, V., et al. In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides 37(1), 86-97 (2012).