Burapitant
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| Clinical data | |
|---|---|
| ATC code | none |
| Identifiers | |
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| CAS Number |
537034-22-3  |
| PubChem (CID) | 23649599 |
| ChemSpider | 26519428 |
| UNII |
E35SK332MS  |
| Chemical and physical data | |
| Formula | C31H35Cl2F6N3O3 |
| Molar mass | 682.524 g/mol |
| 3D model (Jmol) | Interactive image |
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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
- ↑ Emonds-Alt X, Proietto V, Steinberg R, Oury-Donat F, Vigé X, Vilain P, Naline E, Daoui S, Advenier C, Le Fur G, Maffrand JP, Soubrié P, Pascal M. 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. J Pharmacol Exp Ther. 2002 Dec;303(3):1171-9. PMID 12438541
- ↑ Steinberg R, Alonso R, Rouquier L, Desvignes C, Michaud JC, Cudennec A, Jung M, Simiand J, Griebel G, Emonds-Alt X, Le Fur G, Soubrié P. 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. J Pharmacol Exp Ther. 2002 Dec;303(3):1180-8. PMID 12438542
- ↑ Pérez S, Tierney A, Deniau JM, Kemel ML. 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. J Neurochem. 2007 Dec;103(6):2153-63. PMID 17949415
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