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RU-24969

Chemical compound

Chemical compound

RU-24,969 is a serotonin receptor modulator of the tetrahydropyridinylindole group related to 5-MeO-DMT which is used in scientific research.

It is a selective agonist of the serotonin 5-HT1A and 5-HT1B receptors, with 5-fold preference for the latter receptor over the former. In studies, its affinities (Ki) were 2nM for the serotonin 5-HT1 receptor, 5nM for the serotonin 5-HT1A receptor, 4nM for the serotonin 5-HT1B receptor, 780 to 1,000nM for the serotonin 5-HT2 receptor, and 400nM for the serotonin 5-HT2C receptor. It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors.

The drug produces MDMA-like locomotor hyperactivity in animals and this is thought to be mediated by activation of both serotonin 5-HT1A and 5-HT1B receptors. As with other serotonin 5-HT1B receptor agonists such as CP-94,253, RU-24,969 has also been found to increase the reinforcing properties of cocaine in animals, suggesting a role for serotonin 5-HT1B receptors in cocaine addiction as well. The drug produces antiaggressive effects in rodents.

RU-24,969 was first described in the scientific literature by 1980.

References

References

  1. (1991). "Biochemistry and Physiology of Substance Abuse". CRC Press.
  2. (1 January 2002). "Behavioral Psychopharmacology of MDMA and MDMA-Like Drugs: A Review of Human and Animal Studies". Informa UK Limited.
  3. (June 1985). "Differential selectivities of RU 24969 and 8-OH-DPAT for the purported 5-HT1A and 5-HT1B binding sites. Correlation between 5-HT1A affinity and hypotensive activity". European Journal of Pharmacology.
  4. (January 1987). "Central serotonin receptors as targets for drug research". J Med Chem.
  5. (1997). "Pharmacochemistry Library". Elsevier.
  6. (February 2020). "Serotonin 5-HT1A and 5-HT1B receptors co-mediate the RU 24969-induced locomotor activity of male and female preweanling rats". Pharmacology, Biochemistry, and Behavior.
  7. (December 2001). "Which neuroreceptors mediate the subjective effects of MDMA in humans? A summary of mechanistic studies". Human Psychopharmacology.
  8. (May 1993). "Serotonin1B receptor activation mimics behavioral effects of presynaptic serotonin release". Neuropsychopharmacology.
  9. (January 1999). "Locomotor response to MDMA is attenuated in knockout mice lacking the 5-HT1B receptor". Psychopharmacology.
  10. (December 1998). "Serotonin1B receptor stimulation enhances cocaine reinforcement". The Journal of Neuroscience.
  11. (1992). "Rodent models of aggressive behavior and serotonergic drugs". Prog Neuropsychopharmacol Biol Psychiatry.
  12. (1993). "The role of serotonergic mechanisms in inhibition of isolation-induced aggression in male mice". Psychopharmacology (Berl).
  13. (October 1995). "Serotonin receptors and animal models of aggressive behavior". Pharmacopsychiatry.
  14. (April 1980). "Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole)". European Journal of Pharmacology.
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5-ht1a-agonists 5-ht1b-agonists 5-ht7-agonists antiaggressive-drugs methoxy-compounds phenol-ethers tetrahydropyridinylindoles
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