Ezlopitant

Ezlopitant
Systematic (IUPAC) name
	(2S,3S)-2-benzhydryl-N-[(5-isopropyl-2-methoxy-phenyl)methyl]quinuclidin-3-amine
Clinical data
Pregnancy cat.	?
Legal status	Uncontrolled
Routes	Oral
Pharmacokinetic data
Excretion	Urine (32%), Feces (51%)
Identifiers
CAS number	147116-64-1
ATC code	None
PubChem	CID 188927
ChemSpider	164166
UNII	3L098A8MPY
ChEMBL	CHEMBL515966
Chemical data
Formula	C31H38N2O
Mol. mass	454.65 g/mol

Ezlopitant (CJ-11,974) is an NK₁ receptor antagonist.^[1]^[2]^[3] It has antiemetic and antinociceptive effects.^[4]^[5] Pfizer was developing ezlopitant for the treatment of irritable bowel syndrome but it appears to have been discontinued.^[1]

References [edit]

^ ^a ^b Evangelista S (October 2001). "Eziopitant. Pfizer". Current Opinion in Investigational Drugs (London, England : 2000) 2 (10): 1441–3. PMID 11890362.
^ Diemunsch P, Grélot L (September 2000). "Potential of substance P antagonists as antiemetics". Drugs 60 (3): 533–46. PMID 11030465.
^ Giardina GA, Gagliardi S, Martinelli M (August 2003). "Antagonists at the neurokinin receptors--recent patent literature". IDrugs : the Investigational Drugs Journal 6 (8): 758–72. PMID 12917772.
^ Tsuchiya M, Fujiwara Y, Kanai Y, et al. (November 2002). "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 66 (3): 144–52. PMID 12372904.
^ Tsuchiya M, Sakakibara A, Yamamoto M (January 2005). "A tachykinin NK1 receptor antagonist attenuates the 4 beta-phorbol-12-myristate-13-acetate-induced nociceptive behaviour in the rat". European Journal of Pharmacology 507 (1-3): 29–34. doi:10.1016/j.ejphar.2004.11.028. PMID 15659291.

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