RU-24,969 explained

RU-24,969 is a serotonergic drug 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.[1] [2] It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors.[3]

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.[4] [5] [6] [7] 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.[8]

RU-24,969 was first described in the scientific literature by 1980.[9]

See also

Notes and References

  1. Martinez-Price D, Krebs-Thomson K, Geyer M . Behavioral Psychopharmacology of MDMA and MDMA-Like Drugs: A Review of Human and Animal Studies . Addiction Research & Theory . Informa UK Limited . 10 . 1 . 1 January 2002 . 1606-6359 . 10.1080/16066350290001704 . 43–67.
  2. Doods HN, Kalkman HO, De Jonge A, Thoolen MJ, Wilffert B, Timmermans PB, Van Zwieten PA . 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 . 112 . 3 . 363–370 . June 1985 . 3160596 . 10.1016/0014-2999(85)90782-4 .
  3. Book: Grailhe R, Boschert U, Hen R . Pharmacochemistry Library . The 5-HT5, 5-HT6 and 5-HT7 receptors . Elsevier . 1997 . 27 . 978-0-444-82041-9 . 0165-7208 . 10.1016/s0165-7208(97)80018-9 . free . 311–323.
  4. McDougall SA, Robinson JA, Ramirez EL, Diaz HA . 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 . 189 . 172857 . February 2020 . 31958472 . 10.1016/j.pbb.2020.172857 .
  5. Liechti ME, Vollenweider FX . Which neuroreceptors mediate the subjective effects of MDMA in humans? A summary of mechanistic studies . Human Psychopharmacology . 16 . 8 . 589–598 . December 2001 . 12404538 . 10.1002/hup.348 .
  6. Rempel NL, Callaway CW, Geyer MA . Serotonin1B receptor activation mimics behavioral effects of presynaptic serotonin release . Neuropsychopharmacology . 8 . 3 . 201–211 . May 1993 . 8099482 . 10.1038/npp.1993.22 .
  7. Scearce-Levie K, Viswanathan SS, Hen R . Locomotor response to MDMA is attenuated in knockout mice lacking the 5-HT1B receptor . Psychopharmacology . 141 . 2 . 154–161 . January 1999 . 9952039 . 10.1007/s002130050819 .
  8. Parsons LH, Weiss F, Koob GF . Serotonin1B receptor stimulation enhances cocaine reinforcement . The Journal of Neuroscience . 18 . 23 . 10078–10089 . December 1998 . 9822762 . 6793270 . 10.1523/JNEUROSCI.18-23-10078.1998 .
  9. Euvrard C, Boissier JR . Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole) . European Journal of Pharmacology . 63 . 1 . 65–72 . April 1980 . 6155275 . 10.1016/0014-2999(80)90117-x .

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