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
NK1receptor.[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
^Emonds-Alt X, Proietto V, Steinberg R, Oury-Donat F, Vigé X, Vilain P, et al. (December 2002). "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.
doi:
10.1124/jpet.102.040162.
PMID12438541.
S2CID1467606.
^Steinberg R, Alonso R, Rouquier L, Desvignes C, Michaud JC, Cudennec A, et al. (December 2002). "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.
doi:
10.1124/jpet.102.040279.
PMID12438542.
S2CID286897.