Chemistry:MS-245

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Short description: Chemical compound
MS-245
MS-245.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC19H22N2O3S
Molar mass358.46 g·mol−1
3D model (JSmol)
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MS-245 is a tryptamine derivative 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. "N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists". Bioorganic & Medicinal Chemistry Letters 10 (20): 2295–9. October 2000. doi:10.1016/S0960-894X(00)00453-4. PMID 11055342. 
  2. "Interaction of chiral MS-245 analogs at h5-HT6 receptors". Bioorganic & Medicinal Chemistry Letters 15 (15): 3510–3. August 2005. doi:10.1016/j.bmcl.2005.05.092. PMID 15990303. 
  3. "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. February 2008. doi:10.1021/jm070910s. PMID 18201064. 
  4. "Modulation of the stimulus effects of (+)amphetamine by the 5-HT6 antagonist MS-245". Pharmacology, Biochemistry, and Behavior 78 (2): 263–8. June 2004. doi:10.1016/j.pbb.2004.03.017. PMID 15219766. 
  5. "Effect of the 5-HT(6) serotonin antagonist MS-245 on the actions of (-)nicotine". Pharmacology, Biochemistry, and Behavior 85 (1): 170–7. September 2006. doi:10.1016/j.pbb.2006.07.029. PMID 16950502.