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RU-24969

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RU-24969
Clinical data
Other namesRU-24969; RU24969
Drug classSerotonin 5-HT1B and 5-HTA receptor agonist
Identifiers
  • 5-Methoxy-3-(1,2,5,6-tetrahydro-4-pyridinyl)-1H-indole
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H16N2O
Molar mass228.295 g·mol−1
3D model (JSmol)
  • c3cc(OC)cc1c3[nH]cc1C=2CCNCC=2
  • InChI=1S/C14H16N2O/c1-17-11-2-3-14-12(8-11)13(9-16-14)10-4-6-15-7-5-10/h2-4,8-9,15-16H,5-7H2,1H3 ☒N
  • Key:KRVMLPUDAOWOGN-UHFFFAOYSA-N ☒N
  (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

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References

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  1. ^ a b c Martinez-Price D, Krebs-Thomson K, Geyer M (1 January 2002). "Behavioral Psychopharmacology of MDMA and MDMA-Like Drugs: A Review of Human and Animal Studies". Addiction Research & Theory. 10 (1). Informa UK Limited: 43–67. doi:10.1080/16066350290001704. ISSN 1606-6359.
  2. ^ a b Doods HN, Kalkman HO, De Jonge A, Thoolen MJ, Wilffert B, Timmermans PB, et al. (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. 112 (3): 363–370. doi:10.1016/0014-2999(85)90782-4. PMID 3160596.
  3. ^ Nichols DE, Oberlender R, McKenna DJ (1991). "Stereochemical Aspects of Hallucinogenesis". In Watson RR (ed.). Biochemistry and Physiology of Substance Abuse. Vol. 3. Boca Raton, Fla.: CRC Press. pp. 1–39. ISBN 978-0-8493-4463-3. OCLC 26748320.
  4. ^ Glennon RA (January 1987). "Central serotonin receptors as targets for drug research". J Med Chem. 30 (1): 1–12. doi:10.1021/jm00384a001. PMID 3543362. Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites
  5. ^ Grailhe R, Boschert U, Hen R (1997). "The 5-HT5, 5-HT6 and 5-HT7 receptors". Pharmacochemistry Library. Vol. 27. Elsevier. pp. 311–323. doi:10.1016/s0165-7208(97)80018-9. ISBN 978-0-444-82041-9. ISSN 0165-7208.
  6. ^ McDougall SA, Robinson JA, Ramirez EL, Diaz HA (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. 189 172857. doi:10.1016/j.pbb.2020.172857. PMID 31958472.
  7. ^ Liechti ME, Vollenweider FX (December 2001). "Which neuroreceptors mediate the subjective effects of MDMA in humans? A summary of mechanistic studies". Human Psychopharmacology. 16 (8): 589–598. doi:10.1002/hup.348. PMID 12404538.
  8. ^ Rempel NL, Callaway CW, Geyer MA (May 1993). "Serotonin1B receptor activation mimics behavioral effects of presynaptic serotonin release". Neuropsychopharmacology. 8 (3): 201–211. doi:10.1038/npp.1993.22. PMID 8099482.
  9. ^ Scearce-Levie K, Viswanathan SS, Hen R (January 1999). "Locomotor response to MDMA is attenuated in knockout mice lacking the 5-HT1B receptor". Psychopharmacology. 141 (2): 154–161. doi:10.1007/s002130050819. PMID 9952039.
  10. ^ Parsons LH, Weiss F, Koob GF (December 1998). "Serotonin1B receptor stimulation enhances cocaine reinforcement". The Journal of Neuroscience. 18 (23): 10078–10089. doi:10.1523/JNEUROSCI.18-23-10078.1998. PMC 6793270. PMID 9822762.
  11. ^ Olivier B, Mos J (1992). "Rodent models of aggressive behavior and serotonergic drugs". Prog Neuropsychopharmacol Biol Psychiatry. 16 (6): 847–870. doi:10.1016/0278-5846(92)90104-m. PMID 1513929.
  12. ^ Sánchez C, Arnt J, Hyttel J, Moltzen EK (1993). "The role of serotonergic mechanisms in inhibition of isolation-induced aggression in male mice". Psychopharmacology (Berl). 110 (1–2): 53–59. doi:10.1007/BF02246950. PMID 7870899.
  13. ^ Olivier B, Mos J, van Oorschot R, Hen R (October 1995). "Serotonin receptors and animal models of aggressive behavior". Pharmacopsychiatry. 28 Suppl 2: 80–90. doi:10.1055/s-2007-979624. PMID 8614705.
  14. ^ Euvrard C, Boissier JR (April 1980). "Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole)". European Journal of Pharmacology. 63 (1): 65–72. doi:10.1016/0014-2999(80)90117-x. PMID 6155275.
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