Ezlopitant  (Synonyms: CJ-11,974)

Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research^[1][2][3].

Ezlopitant (CJ-11,974) is converted to two pharmacologically active metabolites: CJ-12458, an alkene metabolite and CJ-12764, a benzylic alcohol^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ezlopitant (CJ-11,974; 2, 5, 10 mg/kg; i.p.; 30 minutes) decreases both sucrose and ethanol operant-self administration in rats^[1].
Pharmacokinetic Parameters of Ezlopitant in Rat, Gerbil, Guinea pig, Ferret, Dog, Monkey ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

454.65

C₃₁H₃₈N₂O

147116-64-1

COC(C=CC(C(C)C)=C1)=C1CN[C@@H](C2CCN3CC2)[C@@H]3C(C4=CC=CC=C4)C5=CC=CC=C5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pia Steensland, et al. The neurokinin 1 receptor antagonist, ezlopitant, reduces appetitive responding for sucrose and ethanol. PLoS One. 2010 Sep 1;5(9):e12527.  [Content Brief]

  [2]. A E Reed-Hagen, et al. Pharmacokinetics of ezlopitant, a novel non-peptidic neurokinin-1 receptor antagonist in preclinical species and metabolite kinetics of the pharmacologically active metabolites. Biopharm Drug Dispos. 1999 Dec;20(9):429-39.  [Content Brief]

  [3]. Megumi Tsuchiya, et al. Anti-emetic activity of the novel nonpeptide tachykinin NK1 receptor antagonist ezlopitant (CJ-11,974) against acute and delayed cisplatin-induced emesis in the ferret. Pharmacology. 2002 Nov;66(3):144-52.  [Content Brief]