Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2 binding affinity
Kurt Rasmussen, Richard A Glennon, George K. Aghajanian
European Journal of Pharmacology December 1, 1986 DOI: 10.1016/0014-2999(86)90014-2 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Locus coeruleus neurons (in vitro) |
| Interventions | DOM SL-7161 |
| Topics | Serotonin |
| Keywords | Phenethylamine Hallucinogen Locus coeruleus Potency 5-ht2 receptor Pharmacology Stereochemistry Biochemistry 5-HT Receptor Central nervous system In vitro |
| Citations | 50 |
| Key findings | The rank order of potency for phenethylamine hallucinogens in the locus coeruleus matches their 5-HT2 binding affinity, and the inactive isomer SL-7161 had no significant effect. |
Abstract
The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2 binding affinity [-) DOB greater than DOM greater than ( + )DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into structure-activity relationships at 5-HT2 receptors and support earlier findings that the actions of hallucinogens displayed in the LC are mediated via 5-HT2 receptors.