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MS-245

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MS-245
Systematic (IUPAC) name
2-[5-methoxy-1-(phenylsulfonyl)-1H-indol-3-yl]-N,N-dimethylethanamine
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number ?
ATC code None
PubChem CID 6918542
Chemical data
Formula C19H22N2O3S 
Mol. mass 358.454 g/mol
SMILES eMolecules & PubChem
 YesY(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]

[edit] See also

[edit] 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. doi:10.1016/S0960-894X(00)00453-4. PMID 11055342. 
  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. doi:10.1016/j.bmcl.2005.05.092. PMID 15990303. 
  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 medicinal chemistry 51 (3): 603–11. doi:10.1021/jm070910s. PMID 18201064. 
  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. doi:10.1016/j.pbb.2004.03.017. PMID 15219766. 
  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. doi:10.1016/j.pbb.2006.07.029. PMID 16950502. 

2-Methyl-5-HT • 4-Acetoxy-DET • 4-Acetoxy-DiPT • 4-Acetoxy-DMT • 4-Acetoxy-MiPT • 4-AcO-MET • 4-HO-αMT • 4-HO-DiPT • 4-HO-MET • 4-MeO-DMT • 4-Methyl-αET • 4-Methyl-αMT • 4,5-DHP-DMT • 4,5-MDO-DMT • 4,5-MDO-DIPT • 5-Benzyloxytryptamine • 5-Bromo-DMT • 5-Carboxamidotryptamine • 5-Ethoxy-αMT • 5-Fluoro-αMT • 5-HO-αMT • 5-HTP • 5-Ethoxy-DMT • 5-Ethyl-DMT • 5-Fluoro-DMT • 5-Methyl-DMT • 5-Methoxytryptamine • 5-MeO-7,N,N-TMT • 5-Methyl-αET • 5-MeO-αET  • 5-MeO-αMT • 5-MeO-DALT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MeO-MALT • 5-MeO-MiPT • 5-MeO-NBpBrT • 5,7-Dihydroxytryptamine • 5-(Nonyloxy)tryptamine • 6-Fluoro-αMT • 7-Methyl-αET • 7-Methyl-DMT • αET • αMT • Aeruginascin • AL-37350A • BW-723C86 • Baeocystin • Bufotenidine • Bufotenin • DALT • Desformylflustrabromine • DET • DiPT • DMT • DPT • Ethocybin • EiPT • EMDT • EPT • Ethocin • FGIN-127 • FGIN-143 • Ibogaine • Indorenate • Iprocin • MET • MiPT • MPT • Miprocin • Melatonin • MS-245 • NAS • NMT • Norbaeocystin • Normelatonin • Oxypertine • PiPT • Psilocin • Psilocybin • Rizatriptan • Serotonin • Sumatriptan • Tryptamine • Tryptophan • Yohimbine • Yuremamine • Zolmitriptan
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