Chemistry:RS134-49
From HandWiki
RS134-49, also known as 4-methyl-THPI, is a tetrahydropyridinylindole (THPI) derivative related to psychedelic tryptamines which acts as a 5-HT2A receptor agonist, with a 5-HT2A Ki of 11.5nM and an EC50 of 22nM. It is a biased agonist selective for activation of the Gq 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]
See also
- Cyclized tryptamine
- Tetrahydropyridinylindole
- RU-28253 (5-MeO-THPI)
- 4-Methyl-AMT
- 4-Methyl-AET
- CP-94253
- RU-24,969
- SN-22
- VU6067416
References
- ↑ "Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment". ACS Medicinal Chemistry Letters 14 (11): 1498–1500. November 2023. doi:10.1021/acsmedchemlett.3c00444. PMID 37974947.
- ↑ 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.", WO patent 2023114472, published 22 June 2023
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