Serotonin Receptor Signaling and Hallucinogenic Drug Action

An oldie but a goodie. This article is of interest because it helps elaborate on the concept that 5-MeO-DMT has high affinity for the serotonin 5-HT1A receptor, and it is 4- to 10-fold more potent than N,N-dimethyltryptamine (DMT) in human subjects” (Shen, H.-W., Jiang, X.-L., Winter, J. C., & Yu, A.-M.). In this article, we can take a look at how various “hallucinogens” also known as psychedelics, entheogens, or medicines affect the serotonergic system in the brain. The article takes a look at the structures of tryptamine, serotonin, psilocin, 5-MeO-DMT, and LSD and also talks about DOI as “hallucinogenic” substances.

From article:
“There are seven known families of serotonin receptors, named 5-HT1 through 5-HT7, encompassing at least 15 subtypes. The classification of receptors relies upon sequence similarity as well as second messenger pathways coupled to receptor activation (reviewed in Gerhardt and Heerikhuizen, 1997). Hallucinogens all have a high affinity for certain serotonin receptor subtypes, namely, the 5-HT2A and 5-HT2C receptor subtypes (Glennon et al, 1984; Sanders-Bush et al, 1988). The relative hallucinogenic potencies of various drugs can be extrapolated by their affinities for these receptors (Glennon et al, 1984).”

Full PDF:

Shen, H.-W., Jiang, X.-L., Winter, J. C., & Yu, A.-M. (2010). Psychedelic 5-Methoxy-N,N-dimethyltryptamine: Metabolism, Pharmacokinetics, Drug Interactions, and Pharmacological Actions. Current Drug Metabolism, 11(8), 659–666.

Posted by: Rafael Lancelotta