| Hazard Information | Back Directory | [Description]
rac-Aprepitant-d4 is intended for use as an internal standard for the quantification of aprepitant (Item No. 14867) by GC- or LC-MS. Aprepitant an antiemetic compound and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).1,2 It is selective for NK1 over NK3 receptors (Ki = 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. | [References]
[1] CATERINA BISSANTZ. 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]. Journal of Medicinal Chemistry, 2012, 55 11: 5061-5076. DOI: 10.1021/jm2017072
[2] PAUL E. FINKE . Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR[J]. Bioorganic & Medicinal Chemistry Letters, 2006, 16 17: Pages 4497-4503. DOI: 10.1016/j.bmcl.2006.06.035
[3] LAURA C. MEURER . Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives[J]. Bioorganic & Medicinal Chemistry Letters, 2006, 16 17: Pages 4504-4511. DOI: 10.1016/j.bmcl.2006.06.044 |
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