Strongest 5-ht2a agonist in psychedelics

Question

Which psychedelic substance is the strongest 5-HT2A agonist?

Marcel · Accepted Answer

The strongest 5-HT₂A agonist among psychedelic substances is 25I-NBOMe. This substance has a particularly low Ki value of 0.044 nM, which indicates a very strong affinity for the 5-HT₂A receptor. This makes 25I-NBOMe one of the most potent known agonists for this receptor compared to other psychedelic substances. Below is a table based on the 5-HT2A affinity from strongest to weakest agonist (lower number = higher affinity) Substance 5-HT₂A Ki (nM) Remarks 25I-NBOMe 0.044 Potent synthetic hallucinogen 25CN-NBOH 0.088 Selective 5-HT₂A agonist (S,S)-DMBMPP 2.5 Structural derivative of 25B-NBOMe LSD 2.9 Classic psychedelic drug Psilocin 6.0 Active metabolite of psilocybin 4-HO-MET 13.0 Synthetic tryptamine 5-MeO-DMT 15–620 Variable affinity depending on the study DMT 127–1,200 Main component of ayahuasca Serotonin 6,500 Endogenous neurotransmitter

Dust	5-HT₂A K_i (nM)	Comments
25I-NBOMe	0,044	Potent synthetic hallucinogen
25CN-NBOH	0,088	Selective 5-HT₂A agonist
(S,S)-DMBMPP	2,5	Structural derivative of 25B-NBOMe
LSD	2,9	Classic psychedelic drug
Psilocin	6,0	Active metabolite of psilocybin
4-HO-MET	13,0	Synthetic tryptamine
5-MeO-DMT	15–620	Variable affinity depending on the study
DMT	127–1,200	Main ingredient of ayahuasca
Serotonin	6.500	Endogenous neurotransmitter

[Solved] Strongest 5-ht2a agonist in psychedelics