Ezlopitant

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

	Rat (IV; 1 mg/kg)	Gerbil (IV; 1 mg/kg)	Guinea pig (IV; 0.2 mg/kg)	Ferret (SC; 0.8 mg/kg)	Dog (IV; 1 mg/kg)	Monkey (IV; 1 mg/kg)
Tmax (h)	5.3	0.3	0.3		0.9	0.8
Cmax (ng/mL)	18	5.98		106	5.98	198
AUC0-∞ (ng∗h/mL)	257	125	35.5	528	634	478
t1/2 (h)	7.7	2.9	0.6	2.2	2.5	5.0
CLp (mL/min/kg)	65	136	98	27	27	42
F (%)	15	2.1		17	28	2.7