MS-245 explained

MS-245 is a tryptamine derivative used in scientific research. It acts as a selective 5-HT₆ receptor antagonist with a K_i 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

• EMDT

Notes and References

1. Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S, Lee M, Glennon RA . 6 . N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists . Bioorganic & Medicinal Chemistry Letters . 10 . 20 . 2295–9 . October 2000 . 11055342 . 10.1016/S0960-894X(00)00453-4 .
2. Abate C, Kolanos R, Dukat M, Setola V, Roth BL, Glennon RA . Bryan Roth. Interaction of chiral MS-245 analogs at h5-HT6 receptors . Bioorganic & Medicinal Chemistry Letters . 15 . 15 . 3510–3 . August 2005 . 15990303 . 10.1016/j.bmcl.2005.05.092 .
3. Dukat M, Mosier PD, Kolanos R, Roth BL, Glennon RA . 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 . 18201064 . 5994921 . 10.1021/jm070910s .
4. Pullagurla M, Bondareva T, Young R, Glennon RA . Modulation of the stimulus effects of (+)amphetamine by the 5-HT6 antagonist MS-245 . Pharmacology, Biochemistry, and Behavior . 78 . 2 . 263–8 . June 2004 . 15219766 . 10.1016/j.pbb.2004.03.017 . 25350474 .
5. Young R, Bondareva T, Wesolowska A, Young S, Glennon RA . 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 . 16950502 . 10.1016/j.pbb.2006.07.029 . 38662192 .