Cayman 13,14-Dihydro Prostaglandin E1; Purity- Greater Than Or Eq

Netupitant is an insurmountable antagonist of the neurokinin-1 (NK₁) receptor (K_i = 0.95 nM in CHO cells expressing the human recombinant receptor). 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. 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.

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