Misplaced Pages

Burapitant

Article snapshot taken from[REDACTED] with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
Chemical compound Pharmaceutical compound
Burapitant
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • 2-acetyl]-2-(3,4-dichlorophenyl)morpholin-2-yl]ethyl]piperidin-4-yl]-2-methylpropanamide
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC31H35Cl2F6N3O3
Molar mass682.53 g·mol
3D model (JSmol)
SMILES
  • CC(C)(C1CCN(CC1)CC2(CN(CCO2)C(=O)CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C4=CC(=C(C=C4)Cl)Cl)C(=O)N
InChI
  • InChI=1S/C31H35Cl2F6N3O3/c1-28(2,27(40)44)20-5-8-41(9-6-20)10-7-29(21-3-4-24(32)25(33)17-21)18-42(11-12-45-29)26(43)15-19-13-22(30(34,35)36)16-23(14-19)31(37,38)39/h3-4,13-14,16-17,20H,5-12,15,18H2,1-2H3,(H2,40,44)/t29-/m0/s1
  • Key:ZLNYUCXXSDDIFU-LJAQVGFWSA-N

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. 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. Emonds-Alt X, Proietto V, Steinberg R, Oury-Donat F, Vigé X, Vilain P, et al. (December 2002). "SSR240600 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. doi:10.1124/jpet.102.040162. PMID 12438541. S2CID 1467606.
  2. Steinberg R, Alonso R, Rouquier L, Desvignes C, Michaud JC, Cudennec A, et al. (December 2002). "SSR240600 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. doi:10.1124/jpet.102.040279. PMID 12438542. S2CID 286897.
  3. Pérez S, Tierney A, Deniau JM, Kemel ML (December 2007). "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" (PDF). Journal of Neurochemistry. 103 (6): 2153–63. doi:10.1111/j.1471-4159.2007.04944.x. PMID 17949415. S2CID 8099165.
Neurokinin receptor modulators
NK1
NK2
NK3
Stub icon

This drug article relating to the nervous system is a stub. You can help Misplaced Pages by expanding it.

Categories:
Burapitant Add topic