147116-64-1
Chemical Structure
Ezlopitant
Synonym(s): CJ-11,974
- CAS No.: 147116-64-1
- Formula:C31H38N2O
- Molecular Weight:454.65
IUPAC Name: (2S,3S)-2-benzhydryl-N-(5-isopropyl-2-methoxybenzyl)quinuclidin-3-amine
InChIKey: XPNMCDYOYIKVGB-CONSDPRKSA-N
SMILES: COC(C=CC(C(C)C)=C1)=C1CN[C@@H](C2CCN3CC2)[C@@H]3C(C4=CC=CC=C4)C5=CC=CC=C5
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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]
Keywords