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.
Comparable studies
Other experimental studies on serotonin, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Psilocybin induces schizophrenia-like psychosis in humans via a serotonin-2 agonist action Healthy human volunteers | 1998 | Experimental study | |
| Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin | 2000 | Experimental study | |
| Methylenedioxyamphetamine (MDA) and methylenedioxymethamphetamine (MDMA) cause selective ablation of serotonergic axon terminals in forebrain: immunocytochemical evidence for neurotoxicity Rat brain | 1988 | Experimental study | |
| The molecular mechanism of "ecstasy" [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Human platelet plasma membrane vesicles and bovine adrenal chromaffin granule membrane... | 1992 | Laboratory study | |
| 5-HT2AReceptor-Mediated Regulation of Brain-Derived Neurotrophic Factor mRNA in the Hippocampus and the Neocortex Rat brain | 1997 | Experimental study |
Citations in the library
Cited by 10
- Pivotal mental states Journal of Psychopharmacology April 1, 2021
- Dihydrobenzofuran Analogues of Hallucinogens. 4. Mescaline Derivatives Journal of Medicinal Chemistry September 1, 1997
- Classic Psychedelic Coadministration with Lithium, but Not Lamotrigine, is Associated with Seizures: An Analysis of Online Psychedelic Experience Reports Pharmacopsychiatry August 4, 2021
- Stimulatory and inhibitory effects of serotonergic hallucinogens on spinal mono- and polysynaptic reflex pathways in the rat. Neuropharmacology July 1, 1992
- Mescaline: excitatory effects on acoustic startle are blocked by serotonin2 antagonists Psychopharmacology November 1, 1987
and 5 more in the library
Cites 3
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- Effect of hallucinogens on spontaneous and sensory-evoked locus coeruleus unit activity in the rat: reversal by selective 5-HT2 antagonists. Brain Research October 1, 1986
- Behavioral and serotonin receptor properties of 4-substituted derivatives of the hallucinogen 1-(2,5-dimethoxyphenyl)-2-aminopropane. Journal of Medicinal Chemistry October 1982