MS-245

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MS-245
(IUPAC) ime
2-[5-metoksi-1-(fenilsulfonil)-1H-indol-3-il]-N,N-dimetiletanamin
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 6918542
Hemijski podaci
Formula C19H22N2O3S 
Mol. masa 358,454 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

MS-245 je triptaminski derivat koji se koristi u naučnim istraživanjima. On deluje kao selektivni antagonist 5-HT6 receptora sa Ki od 2,3 nM. On je izvden putem proučavanja odnosa strukture i aktivnosti selektivnih 5-HT6 agonista EMDT klase.[3] On je korišten kao vodeće jedinjenje za dalji razvoj 5-HT6 antagonista sa triptaminskom osnovom.[4][5] U životinjskim studijama je pokazano pojava aktivnost, mada ne zamenjuje, amfetamin i nikotin.[6][7]

Reference[uredi - уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. 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. 
  4. 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. 
  5. 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. doi:10.1021/jm070910s. PMID 18201064. 
  6. 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. 
  7. 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. 

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