Chemistry:RU-24969

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Short description: Chemical compound

RU-24969
File:5-methoxy-3-(1,2,5,6-tetrahydro-4-pyridinyl)-1H-indole.svg
File:RU-24969 3D.png
Clinical data
Other namesRU-24969; RU24969
Drug classSerotonin 5-HT1B and 5-HTA receptor agonist
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC14H16N2O
Molar mass228.295 g·mol−1
3D model (JSmol)
  (verify)

RU-24,969 is a serotonin receptor modulator of the tetrahydropyridinylindole group related to 5-MeO-DMT which is used in scientific research.[1][2][3]

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] In studies, its affinities (Ki) were 2 nM for the serotonin 5-HT1 receptor, 5 nM for the serotonin 5-HT1A receptor, 4 nM for the serotonin 5-HT1B receptor, 780 to 1,000 nM for the serotonin 5-HT2 receptor, and 400 nM for the serotonin 5-HT2C receptor.[4] It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors.[5]

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.[6][1][7][8][9] 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.[10] The drug produces antiaggressive effects in rodents.[11][12][13]

RU-24,969 was first described in the scientific literature by 1980.[14]

See also

References

  1. ↑ 1.0 1.1 1.2 "Behavioral Psychopharmacology of MDMA and MDMA-Like Drugs: A Review of Human and Animal Studies". Addiction Research & Theory (Informa UK Limited) 10 (1): 43–67. 1 January 2002. doi:10.1080/16066350290001704. ISSN 1606-6359. 
  2. ↑ 2.0 2.1 "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. doi:10.1016/0014-2999(85)90782-4. PMID 3160596. 
  3. ↑ "Stereochemical Aspects of Hallucinogenesis". Biochemistry and Physiology of Substance Abuse. 3. Boca Raton, Fla.: CRC Press. 1991. pp. 1–39. ISBN 978-0-8493-4463-3. OCLC 26748320. https://bitnest.netfirms.com/external/Books/BiochemistryPhysiologySubstanceAbuse3.1. 
  4. ↑ "Central serotonin receptors as targets for drug research". J Med Chem 30 (1): 1–12. January 1987. doi:10.1021/jm00384a001. PMID 3543362. "Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites". 
  5. ↑ "The 5-HT5, 5-HT6 and 5-HT7 receptors". Pharmacochemistry Library. 27. Elsevier. 1997. pp. 311–323. doi:10.1016/s0165-7208(97)80018-9. ISBN 978-0-444-82041-9. 
  6. ↑ "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. February 2020. doi:10.1016/j.pbb.2020.172857. PMID 31958472. 
  7. ↑ "Which neuroreceptors mediate the subjective effects of MDMA in humans? A summary of mechanistic studies". Human Psychopharmacology 16 (8): 589–598. December 2001. doi:10.1002/hup.348. PMID 12404538. 
  8. ↑ "Serotonin1B receptor activation mimics behavioral effects of presynaptic serotonin release". Neuropsychopharmacology 8 (3): 201–211. May 1993. doi:10.1038/npp.1993.22. PMID 8099482. 
  9. ↑ "Locomotor response to MDMA is attenuated in knockout mice lacking the 5-HT1B receptor". Psychopharmacology 141 (2): 154–161. January 1999. doi:10.1007/s002130050819. PMID 9952039. 
  10. ↑ "Serotonin1B receptor stimulation enhances cocaine reinforcement". The Journal of Neuroscience 18 (23): 10078–10089. December 1998. doi:10.1523/JNEUROSCI.18-23-10078.1998. PMID 9822762. 
  11. ↑ "Rodent models of aggressive behavior and serotonergic drugs". Prog Neuropsychopharmacol Biol Psychiatry 16 (6): 847–870. 1992. doi:10.1016/0278-5846(92)90104-m. PMID 1513929. 
  12. ↑ "The role of serotonergic mechanisms in inhibition of isolation-induced aggression in male mice". Psychopharmacology (Berl) 110 (1-2): 53–59. 1993. doi:10.1007/BF02246950. PMID 7870899. 
  13. ↑ "Serotonin receptors and animal models of aggressive behavior". Pharmacopsychiatry 28 Suppl 2: 80–90. October 1995. doi:10.1055/s-2007-979624. PMID 8614705. 
  14. ↑ "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. doi:10.1016/0014-2999(80)90117-x. PMID 6155275. 



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