Open Access Articles- Top Results for MS-245


File:MS-245 structure.png
Systematic (IUPAC) name
Clinical data
? 7pxY
PubChem CID 6918542
ChemSpider 5293739
Chemical data
Formula C19H22N2O3S
358.454 g/mol
 14pxY (what is this?)  (verify)

MS-245 is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor antagonist with a Ki of 2.3 nM, and was derived through structure-activity relationship development of the selective 5-HT6 agonist EMDT.[1] It has been used as a lead compound for further development of tryptamine-derived 5-HT6 antagonists.[2][3] In animal studies it has been shown to boost the activity of, but not substitute for, both amphetamine and nicotine.[4][5]

See also


  1. ^ Tsai, Y; Dukat, M; Slassi, A; MacLean, N; Demchyshyn, L; Savage, JE; Roth, BL; Hufesein, S et al. (October 2000). "N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists". Bioorganic & Medicinal Chemistry Letters 10 (20): 2295–9. PMID 11055342. doi:10.1016/S0960-894X(00)00453-4. 
  2. ^ Abate, C; Kolanos, R; Dukat, M; Setola, V; Roth, BL; Glennon, RA (August 2005). "Interaction of chiral MS-245 analogs at h5-HT6 receptors". Bioorganic & Medicinal Chemistry Letters 15 (15): 3510–3. PMID 15990303. doi:10.1016/j.bmcl.2005.05.092. 
  3. ^ Dukat, M; Mosier, PD; Kolanos, R; Roth, BL; Glennon, RA (February 2008). "Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies". Journal of Medical Chemistry 51 (3): 603–11. PMID 18201064. doi:10.1021/jm070910s. 
  4. ^ Pullagurla, M; Bondareva, T; Young, R; Glennon, RA (June 2004). "Modulation of the stimulus effects of (+)amphetamine by the 5-HT6 antagonist MS-245". Pharmacology, Biochemistry, and Behavior 78 (2): 263–8. PMID 15219766. doi:10.1016/j.pbb.2004.03.017. 
  5. ^ Young, R; Bondareva, T; Wesolowska, A; Young, S; Glennon, RA (September 2006). "Effect of the 5-HT(6) serotonin antagonist MS-245 on the actions of (-)nicotine". Pharmacology, Biochemistry, and Behavior 85 (1): 170–7. PMID 16950502. doi:10.1016/j.pbb.2006.07.029.