MS-245

MS-245
(IUPAC) ime
	2-[5-metoksi-1-(fenilsulfonil)-1H-indol-3-il]-N,N-dimetiletanamin
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	6918542
Hemijski podaci
Formula	C19H22N2O3S
Mol. masa	358,454 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H22N2O3S/c1-20(2)12-11-15-14-21(19-10-9-16(24-3)13-18(15)19)25(22,23)17-7-5-4-6-8-17/h4-10,13-14H,11-12H2,1-3H3 ; Key: AIJIQCBYMBZLJD-UHFFFAOYSA-N
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 K_i 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

↑ 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
↑ 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.

Povezano

EMDT

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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 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.

[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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