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RS-102221

Chemical compound

Chemical compound

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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-HT2C receptor, with around 100× selectivity over the closely related 5-HT2A and 5-HT2B receptors. It has anxiolytic effects in animal studies, increases the effectiveness of SSRI antidepressants, and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT2C receptor in regulation of the dopamine signalling system in the brain.

References

References

  1. (1997). "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology.
  2. (July 2006). "Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior". Bulletin of Experimental Biology and Medicine.
  3. (October 2004). "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology.
  4. (April 2002). "Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus effects of cocaine". Pharmacology, Biochemistry, and Behavior.
  5. (August 2003). "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.
  6. (September 2005). "Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities". Brain Research.
  7. (February 2006). "Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response". Current Drug Targets.
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