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

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]

See also

References

  1. ^ a b Evangelista S (October 2001). "Eziopitant. Pfizer". Current Opinion in Investigational Drugs (London, England : 2000) 2 (10): 1441–3. PMID 11890362. 
  2. ^ Diemunsch P, Grélot L (September 2000). "Potential of substance P antagonists as antiemetics". Drugs 60 (3): 533–46. PMID 11030465. http://content.wkhealth.com/linkback/openurl?issn=0012-6667&volume=60&issue=3&spage=533. 
  3. ^ 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. 
  4. ^ 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. http://content.karger.com/produktedb/produkte.asp?typ=fulltext&file=pha66144. 
  5. ^ 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. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(04)01326-3. 
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