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RS134-49

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
RS134-49
Clinical data
Other names4-Methyl-THPI; 4-Me-THPI
Identifiers
  • 4-methyl-3-(1,2,3,6-tetrahydropyridin-5-yl)-1H-indole
CAS Number
PubChemCID
Chemical and physical data
FormulaC14H16N2
Molar mass212.296 g·mol−1
3D model (JSmol)
  • CC1=C2C(=CC=C1)NC=C2C3=CCCNC3
  • InChI=1S/C14H16N2/c1-10-4-2-6-13-14(10)12(9-16-13)11-5-3-7-15-8-11/h2,4-6,9,15-16H,3,7-8H2,1H3
  • Key:UIZDBLDTIJHWHC-UHFFFAOYSA-N

RS134-49, also known as4-methyl-THPI, is atetrahydropyridinylindole (THPI) derivative related topsychedelictryptamines which acts as a5-HT2A receptor agonist, with a 5-HT2A Ki of 11.5nM and an EC50 of 22nM. It is abiased agonist selective for activation of theGq coupled signalling pathway with weaker activation of theβ-arrestin 2 coupled pathway, but shows a more balanced profile than related compounds such as(R)-69.[1][2]

See also

[edit]

References

[edit]
  1. ^Kargbo RB (November 2023)."Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment".ACS Medicinal Chemistry Letters.14 (11):1498–1500.doi:10.1021/acsmedchemlett.3c00444.PMC 10641896.PMID 37974947.
  2. ^WO 2023114472, Manish J, Slocum S, Skiniotis G, Barros X, Jin J, Kaniskan HU, Sun N, Xiong Y, Shen Y, Xu Z, Qui X, Qian C, Song X, Deng Z, Roth B, Biberto J, Kuglae K, Suomivuori CM, Daemgen MA, Dror R, Shoichet B, Kaplan AL, "Heterocyclic compounds as 5ht2a biased agonists.", published 22 June 2023, assigned to Icahn School of Medicine at Mount Sinai, The University of North Carolina at Chapel Hill, The Board of Trustees of The Leland Stanford Junior University, The Regents of The University of California 
Tryptamines
4-Hydroxytryptamines
andesters/ethers
5-Hydroxy- and
5-methoxytryptamines
N-Acetyltryptamines
α-Alkyltryptamines
Cyclized tryptamines
Isotryptamines
Related compounds


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