Chemistry:Burapitant

From HandWiki
Short description: Chemical compound
Burapitant
Burapitant structure.png
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC31H35Cl2F6N3O3
Molar mass682.53 g·mol−1
3D model (JSmol)

Burapitant (SSR-240,600) is a drug developed by Sanofi-Aventis which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor.[1][2][3] While burapitant itself did not proceed beyond early clinical trials and was never developed for clinical use in humans, promising animal results from this and related compounds have led to a number of novel drugs from this class that have now been introduced into medical use.

References

  1. "SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization". The Journal of Pharmacology and Experimental Therapeutics 303 (3): 1171–9. December 2002. doi:10.1124/jpet.102.040162. PMID 12438541. 
  2. "SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]-4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin 1 receptor: II. Neurochemical and behavioral characterization". The Journal of Pharmacology and Experimental Therapeutics 303 (3): 1180–8. December 2002. doi:10.1124/jpet.102.040279. PMID 12438542. 
  3. "Tachykinin regulation of cholinergic transmission in the limbic/prefrontal territory of the rat dorsal striatum: implication of new neurokinine 1-sensitive receptor binding site and interaction with enkephalin/mu opioid receptor transmission". Journal of Neurochemistry 103 (6): 2153–63. December 2007. doi:10.1111/j.1471-4159.2007.04944.x. PMID 17949415. https://www.hal.inserm.fr/inserm-00165788/file/Perez_et_al.pdf.