MS-245
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| |||
| (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 | uredi kod]
- ↑ 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.
- ↑ 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.
- ↑ Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S i dr.. (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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
