Hallucinogenic drug interactions with neurotransmitter receptor binding sites in human cortex.
Psychopharmacology 1989 DOI: 10.1007/bf00443425 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro binding affinity study Peer reviewed |
|---|---|
| Population | Human cortex tissue |
| Interventions | d-Lysergic acid diethylamide (d-LSD) N N-dimethyltryptamine (DMT) 1-(2 5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) 5-dimethoxy-4-bromophenyl)-2-aminopropane (DOB) |
| Key points | All four hallucinogens bound most strongly to the "DOB binding site" labeled by 77Br-R(-)DOB, with DOI and DOB in the subnanomolar range and d-LSD and DMT in the nanomolar range. d-LSD was the most potent at six of the other eight sites, and all four bound the 5-HT2 receptor with potencies of 4 to 360 nM. The authors propose that these affinity differences account for the agents' differing effects in biochemical and physiological assays. |
Abstract
The binding affinities of four hallucinogenic agents were analyzed at nine neurotransmitter binding sites in human cortex. d-Lysergic acid diethylamide (d-LSD), N,N-dimethyltryptamine (DMT), 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane (DOB) display highest affinity for the recently identified "DOB binding site" labeled by 77Br-R(-)DOB. The phenalkylamines, DOI and DOB, display subnanomolar affinity for the 77Br-R(-)DOB-labeled site, whereas the indolealkylamines, d-LSD and DMT, display nanomolar affinity for this site. d-LSD was the most potent of the four hallucinogens at six of the other eight sites analyzed in this study. All four hallucinogens also display high affinity for the 5-hydroxytryptamine2 (5-HT2) receptor subtype, with potencies ranging from 4 to 360 nM. Marked differences in relative affinities were observed between the indolealkylamines and the phenalkylamines at the 5-HT1A, 5-HT1D, and DOB binding sites. These rank-order differences in affinities are likely to account for the differing effects of these agents in various biochemical and physiological assays.