Aprepitant

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK₁) receptor (K_i = 3 nM; IC₅₀ = 0.09 nM for the human receptor).^1,2 It is selective for NK₁ over NK₃ receptors (K_i = 454.1 nM for human NK₃).¹ In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P (Item No. 24035).³ It also reduces NK₁-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.

WARNING This product is not for human or veterinary use.

1. Bissantz, C., Bohnert, C., Hoffmann, T., et al. Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists. J. Med. Chem. 55(11), 5061-5076 (2012).

2. Finke, P.E., Meurer, L.C., Levorse, D.A., et al. Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR. Bioorg. Med. Chem. Lett. 16(17), 4497-4503 (2006).

3. Meurer, L.C., Finke, P.E., Owens, K.A., et al. Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives. Bioorg. Med. Chem. Lett. 16(17), 4504-4511 (2006).