WY-46824

WY-46824 is a norepinephrine-dopamine reuptake inhibitor related to venlafaxine that was disclosed by Paige Mahaney, et al. of Wyeth in 2008.[1] The compound actually appears in an article a year earlier in 2007 but is not the main focus of the work.[2] It has NET binding of 46 nM, DAT = 58 nM and SERT = 18795 nM. The racemic compound was resolved into its constituent enantiomers, and the (S) enantiomer is the more active one. The N-desmethyl derivative shows similar activity.

WY-46824
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H29ClN2O
Molar mass336.89936 g/mol g·mol−1
3D model (JSmol)

References
  1. Mahaney, P.; Gavrin, L.; Trybulski, E.; Stack, G.; Vu, T.; Cohn, S.; Ye, F.; Belardi, J.; Santilli, A.; Sabatucci, J.; Leiter, J.; Johnston, G. H.; Bray, J. A.; Burroughs, K. D.; Cosmi, S. A.; Leventhal, L.; Koury, E. J.; Zhang, Y.; Mugford, C. A.; Ho, D. M.; Rosenzweig-Lipson, S. J.; Platt, B.; Smith, V. A.; Deecher, D. C. (2008). "Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors". Journal of Medicinal Chemistry. 51 (13): 4038–4049. doi:10.1021/jm8002262. PMID 18557608.
  2. Mason, J. N.; Deecher, D. C.; Richmond, R. L.; Stack, G.; Mahaney, P. E.; Trybulski, E.; Winneker, R. C.; Blakely, R. D. (2007). "Desvenlafaxine Succinate Identifies Novel Antagonist Binding Determinants in the Human Norepinephrine Transporter". Journal of Pharmacology and Experimental Therapeutics. 323 (2): 720–729. doi:10.1124/jpet.107.125716. PMID 17673606.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.