MS-245

MS-245

MS-245
Systematic (IUPAC) name
2-[5-methoxy-1-(phenylsulfonyl)-1H-indol-3-yl]-N,N-dimethylethanamine
Clinical data
Legal status
?
Identifiers
CAS number  YesY
ATC code None
PubChem
ChemSpider
Chemical data
Formula C19H22N2O3S 
Mol. mass 358.454 g/mol
 YesY   

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

References

  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.  
  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.  
  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.  
  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.  
  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.