Chemistry:RU-28253

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RU-28253, also known as 5-MeO-THPI, is a non-selective serotonin receptor agonist of the tryptamine, 5-methoxytryptamine, and tetrahydropyridinylindole families.[1][2][3][4] It is a tetrahydropyridylindole and a conformationally constrained analogue of 5-MeO-DMT.[2][3]

The drug shows high affinity for the serotonin 5-HT1A receptor (Ki = 5.7 nM) and lower affinity for the serotonin 5-HT2A receptor (Ki = 230 nM).[2] Its affinities for these receptors were higher than those of dimethyltryptamine (DMT).[2] RU-28253 is described as a potent agonist of the serotonin 5-HT1 and 5-HT2 receptors,[5] including of the serotonin 5-HT1B receptor,[6] and is also an agonist of the serotonin 5-HT4 receptor.[3][7]

RU-28253 was first described in the scientific literature by 1983.[8][9][2]

See also

References

  1. ↑ "5-hydroxytryptamine (5-HT) receptor ligands". Current Pharmaceutical Design 13 (25): 2621–2637. 2007. doi:10.2174/138161207781663000. PMID 17897004. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "Relative selectivity of some conformationally constrained tryptamine analogs at 5-HT1, 5-HT1A and 5-HT2 recognition sites". Life Sciences 41 (16): 1961–1969. October 1987. doi:10.1016/0024-3205(87)90749-1. PMID 3657392. 
  3. ↑ 3.0 3.1 3.2 Dean RL (1999). Conformationally and rotationally restricted analogs of 5-hydroxytryptamine (Ph.D. thesis). University of Arizona. ProQuest 304510409. Retrieved 1 April 2025. Tetrahydropyridylindoles have been of interest since the initial reports showed that RU 24969 (6) and RU 28253 (7) had high potency as 5-HT agonists and were able to differentiate between certain 5-HT receptors (Euvard, 1980; Hunt, 1981). [...] RU 28253 acts as an agonist at the 5-HT4 receptor, having selective activity over RU 24969. [...]
  4. ↑ "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. 
  5. ↑ "Synthesis and serotonin receptor binding properties of 5-substituted 3-(1′,2′,5′,6′-tetrahydropyridin-3′-yl) indoles". Bioorganic & Medicinal Chemistry Letters 5 (24): 2963–2968. 1995. doi:10.1016/0960-894X(95)00534-8. 
  6. ↑ "A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system". Molecular Pharmacology 34 (6): 880–887. December 1988. doi:10.1016/S0026-895X(25)10130-2. PMID 2849052. 
  7. ↑ "5-HT4 receptors". Pharmacochemistry Library. 27. Elsevier. 1997. pp. 261–308. doi:10.1016/s0165-7208(97)80017-7. ISBN 978-0-444-82041-9. 
  8. ↑ "Poster Communications: Part I: The Actions of Three Mammalian Serotonin Receptor Agonists on Helix Central Neurones". British Journal of Pharmacology 80 (Suppl): 494P–533P. 1983. 
  9. ↑ Taylor EW (1985). The Development of Indoleamine Derivatives (Ph.D. thesis). University of Arizona. ProQuest 303387893. Retrieved 1 April 2025.



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