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RU-28253

From Wikipedia, the free encyclopedia

Pharmaceutical compound
RU-28253
Clinical data
Other namesRU28253
Drug classNon-selectiveserotonin receptor agonist
Identifiers
  • 5-methoxy-3-(1,2,3,6-tetrahydropyridin-5-yl)-1H-indole
PubChemCID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC14H16N2O
Molar mass228.295 g·mol−1
3D model (JSmol)
  • COC1=CC2=C(C=C1)NC=C2C3=CCCNC3
  • InChI=1S/C14H16N2O/c1-17-11-4-5-14-12(7-11)13(9-16-14)10-3-2-6-15-8-10/h3-5,7,9,15-16H,2,6,8H2,1H3
  • Key:WBJMGSVSSCEGFV-UHFFFAOYSA-N

RU-28253 is anon-selectiveserotonin receptor agonist of thetryptamine and5-methoxytryptamine families.[1][2][3] It is a tetrahydropyridylindole and aconformationally constrainedanalogue of5-MeO-DMT.[2][3] The drug shows highaffinity for theserotonin5-HT1A receptor (Ki = 5.7 nM) and lower affinity for the serotonin5-HT2A receptor (Ki = 230 nM).[2] Its affinities for these receptors were higher than those ofdimethyltryptamine (DMT).[2] The drug is described as apotent agonist of the serotonin5-HT1 and5-HT2 receptors,[4] including of the serotonin5-HT1B receptor,[5] and is also an agonist of the serotonin5-HT4 receptor.[3][6] RU-28253 was first described in thescientific literature by 1983.[7][8][2]

See also

[edit]

References

[edit]
  1. ^Kitson SL (2007). "5-hydroxytryptamine (5-HT) receptor ligands".Current Pharmaceutical Design.13 (25):2621–2637.doi:10.2174/138161207781663000.PMID 17897004.
  2. ^abcdeTaylor EW, Nikam S, Weck B, Martin A, Nelson D (October 1987). "Relative selectivity of some conformationally constrained tryptamine analogs at 5-HT1, 5-HT1A and 5-HT2 recognition sites".Life Sciences.41 (16):1961–1969.doi:10.1016/0024-3205(87)90749-1.PMID 3657392.
  3. ^abcDean RL (1999).Conformationally and rotationally restricted analogs of 5-hydroxytryptamine (Ph.D. thesis). University of Arizona.ProQuest 304510409. Retrieved1 April 2025 – via ProQuest.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. ^Dahlgren T, Dean RL, Gharat LA, Johansson AM, Lambert G, Li HB, et al. (1995). "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.doi:10.1016/0960-894X(95)00534-8.
  5. ^Dumuis A, Bouhelal R, Sebben M, Cory R, Bockaert J (December 1988). "A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system".Molecular Pharmacology.34 (6):880–887.doi:10.1016/S0026-895X(25)10130-2.PMID 2849052.
  6. ^Dumuis A, Ansanay H, Waeber C, Sebben M, Fagni L, Bockaert J (1997). "5-HT4 receptors".Pharmacochemistry Library. Vol. 27. Elsevier. pp. 261–308.doi:10.1016/s0165-7208(97)80017-7.ISBN 978-0-444-82041-9.
  7. ^Marrs TC (1983)."Poster Communications: Part I: The Actions of Three Mammalian Serotonin Receptor Agonists on Helix Central Neurones".British Journal of Pharmacology.80 (Suppl):494P –533P.PMC 2044929.
  8. ^Taylor EW (1985).The Development of Indoleamine Derivatives (Ph.D. thesis). University of Arizona.ProQuest 303387893. Retrieved1 April 2025 – via ProQuest.

External links

[edit]
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Tryptamines
4-Hydroxytryptamines
andesters/ethers
5-Hydroxy- and
5-methoxytryptamines
N-Acetyltryptamines
α-Alkyltryptamines
Triptans
Cyclized tryptamines
Isotryptamines
Related compounds
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