RS134-49

RS134-49
Identifiers

IUPAC name 4-methyl-3-(1,2,3,6-tetrahydropyridin-5-yl)-1H-indole
PubChem CID	168941768
Chemical and physical data
Formula	C₁₄H₁₆N₂
Molar mass	212.296 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=C2C(=CC=C1)NC=C2C3=CCCNC3
InChI 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 is a tetrahydropyridine derivative related to psychedelic tryptamines which acts as a 5-HT_2A receptor agonist, with a 5-HT_2A K_i of 11.5nM and an EC₅₀ of 22nM. It is a biased agonist selective for activation of the G_q coupled signalling pathway with weaker activation of the β-arrestin 2 coupled pathway, but shows a more balanced profile than related compounds such as (R)-69.^[1]^[2]

References

^ 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.
^ 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

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References