Chemistry:Ezlopitant

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Short description: Chemical compound
Ezlopitant
Ezlopitant.svg
Clinical data
Other namesCJ-11,974; (2S,3S)-2-Diphenylmethyl-3-[(5-isopropyl-2-methoxybenzyl)amino]quinuclidine[1]
Routes of
administration
By mouth
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Pharmacokinetic data
ExcretionUrine (32%), Feces (51%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC31H38N2O
Molar mass454.658 g·mol−1
3D model (JSmol)

Ezlopitant (INN,[1] code name CJ-11,974) is an NK1 receptor antagonist.[2][3][4] It has antiemetic and antinociceptive effects.[5][6] Pfizer was developing ezlopitant for the treatment of irritable bowel syndrome but it appears to have been discontinued.[2]

See also

  • NK1 receptor antagonist
  • Maropitant (tert-butyl instead of isopropyl)

References

  1. 1.0 1.1 "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 44". World Health Organization. pp. 194–5. https://www.who.int/medicines/publications/druginformation/innlists/RL44.pdf. 
  2. 2.0 2.1 Evangelista S (October 2001). "Eziopitant. Pfizer". Current Opinion in Investigational Drugs 2 (10): 1441–3. PMID 11890362. 
  3. "Potential of substance P antagonists as antiemetics". Drugs 60 (3): 533–46. September 2000. doi:10.2165/00003495-200060030-00002. PMID 11030465. 
  4. "Antagonists at the neurokinin receptors--recent patent literature". IDrugs: The Investigational Drugs Journal 6 (8): 758–72. August 2003. PMID 12917772. 
  5. "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. November 2002. doi:10.1159/000063796. PMID 12372904. http://content.karger.com/produktedb/produkte.asp?typ=fulltext&file=pha66144. 
  6. "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. January 2005. doi:10.1016/j.ejphar.2004.11.028. PMID 15659291.