Aprepitant
Aprepitant is an inhibitor of the tachykinin/neurokinin 1 (NK1) receptor that acts as an antiemetic or anti-nausea medicine. Aprepitant also exhibits some anticancer chemotherapeutic and anti-angiogenic benefit through its inhibition of NK1 receptors, preventing binding of substance P and inhibiting substance P’s proliferative and pro-angiogenic signaling cascade. This compound may also display some antidepressant activity, although in vivo and clinical results have been mixed.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18841982
| Cas No. |
170729-80-3 |
|---|---|
| Purity |
≥98% |
| Formula |
C23H21F7N4O3 |
| Formula Wt. |
534.43 |
| Chemical Name |
5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one |
| IUPAC Name |
5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one |
| Synonym |
(2R)-[(1R)-3,5-bis(trifluoromethyl)phenylethoxy]-(3S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methyl morpholine |
| Melting Point |
255°C |
| Appearance |
White to off white crystalline powder |
Muñoz M, Martinez-Armesto J, Coveñas R. NK-1 receptor antagonists as antitumor drugs: a survey of the literature from 2000 to 2011. Expert Opin Ther Pat. 2012 Jul;22(7):735-46. PMID: 22697287.
Massaro AM, Lenz KL. Aprepitant: a novel antiemetic for chemotherapy-induced nausea and vomiting. Ann Pharmacother. 2005 Jan;39(1):77-85. PMID: 15562136.
Kramer MS, Cutler N, Feighner J, et al. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science. 1998 Sep 11;281(5383):1640-5. PMID: 9733503.
