(R)-69
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PubChem CID | |
Chemical and physical data | |
Formula | C13H15N3 |
Molar mass | 213.284 g·mol−1 |
3D model (JSmol) | |
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(R)-69 (3IQ) is a tetrahydropyridine derivative which acts as a 5-HT2A receptor agonist, with 4.6x selectivity over 5-HT2B and 49x selectivity over 5-HT2C. It has a 5-HT2A Ki of 680nM and an EC50 of 41nM. (R)-69 is a biased agonist selective for activation of the Gq coupled signalling pathway, with much weaker activation of the β-arrestin 2 coupled pathway. In animal studies it produces antidepressant-like activity but without producing the head-twitch response associated with psychedelic effects.[1]
See also
References
- ^ Kaplan AL, Confair DN, Kim K, Barros-Álvarez X, Rodriguiz RM, Yang Y, et al. (September 2022). "Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity". Nature. 610 (7932): 582–591. Bibcode:2022Natur.610..582K. doi:10.1038/s41586-022-05258-z. PMC 9996387. PMID 36171289. S2CID 252598838.
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