RS-102221 explained

RS-102221 is a drug developed by Hoffmann–La Roche, which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT_2C receptor, with around 100× selectivity over the closely related 5-HT_2A and 5-HT_2B receptors.^[1] It has anxiolytic effects in animal studies,^[2] increases the effectiveness of SSRI antidepressants,^[3] and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT_2C receptor in regulation of the dopamine signalling system in the brain.^{[4] [5] [6] [7]}

See also

• CEPC
• SB-242084
• Hydantoin

Notes and References

1. Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW, Flippin LA, Eglen RM . 6 . RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist . Neuropharmacology . 36 . 4–5 . 621–9 . 9225287 . 10.1016/s0028-3908(97)00049-x . 1997 . 24930608 .
2. Kuznetsova EG, Amstislavskaya TG, Shefer EA, Popova NK . Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior . Bulletin of Experimental Biology and Medicine . 142 . 1 . 76–9 . July 2006 . 17369908 . 10.1007/s10517-006-0296-8 . 36424571 .
3. Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, Honig G, Bøgesø KP, Westerink BH, den Boer H, Wikstrom HV, Tecott LH . 6 . Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade . Neuropsychopharmacology . 29 . 10 . 1782–9 . October 2004 . 15138437 . 10.1038/sj.npp.1300474 . free .
4. Filip M, Cunningham KA . Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus effects of cocaine . Pharmacology, Biochemistry, and Behavior . 71 . 4 . 745–56 . April 2002 . 11888566 . 10.1016/s0091-3057(01)00741-9 . 292398 .
5. Filip M, Cunningham KA . Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex . The Journal of Pharmacology and Experimental Therapeutics . 306 . 2 . 734–43 . August 2003 . 12721337 . 10.1124/jpet.102.045716 . 8338748 .
6. Morita K, Hamamoto M, Arai S, Kitayama S, Irifune M, Kawahara M, Kihira K, Dohi T . 6 . Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities . Brain Research . 1057 . 1–2 . 153–60 . September 2005 . 16125150 . 10.1016/j.brainres.2005.07.049 . 30437231 .
7. Dremencov E, Weizmann Y, Kinor N, Gispan-Herman I, Yadid G . Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response . Current Drug Targets . 7 . 2 . 165–75 . February 2006 . 16475958 . 10.2174/138945006775515491 .