Local Cerebral Glucose Utilisation Following Indoleamine‐ and Piperazine‐Containing 5‐Hydroxytryptamine Agonists
Abstract
Abstract: Substances with varying structural components have been shown to have 5‐hydroxytryptamine (5‐HT)‐like properties in the CNS. In this study, putative 5‐HT agonists with indoleamine moeities—lysergic acid diethylamide (LSD) and 5‐methoxy‐N,N‐dimethyltryptamine (5‐MeODMT)—and with piperazine moeities—quipazine (Quip) and 6‐chloro‐2‐(1‐piperazinyl)pyrazine (6‐CPP) were administered to rats. Local cerebral glucose utilisation was measured using the [14 C]2‐deoxyglucose autoradiographic technique. It was found that in most cerebral structures, these substances produced dose‐dependent reductions in glucose utilisation. However, Quip and 6‐CPP increased glucose utilisation in specific areas of the diencephalon (e.g., nucleus reuniens) and produced a biphasic effect in some but not all extrapyramidal structures (e.g., ventromedial caudate nucleus). No such increases in local cerebral glucose utilisation were measured following LSD or 5‐MeODMT administration. These results indicate that although similarities exist between the effects of indoleamine‐ and piperazine‐containing 5‐HT agonists on local cerebral glucose utilisation there are also significant differences in the overall patterns of response produced.
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In that study, treatment with 5-MeO-DMT (0.2 or 2 mg/kg, i.v.) provoked similar patterns of reduced CMRglc, although generally of lower magnitude than the reductions seen with LSD.
“In that study, treatment with 5-MeO-DMT (15, 0.2 or 2 mg/kg, i.v.) provoked similar patterns of reduced CMRglc, although generally of lower magnitude than the reductions seen with LSD (1).”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [134]
Administration to awake (but immobilized) rats of LSD (15 or 150 μg/kg, i.v.) evoked widespread 10-30% reductions in CMRglc, notably throughout neocortex, and in thalamus, lateral geniculate, basal ganglia, and raphé nuclei, but with little effect in cerebellum.
“Administration to awake (but immobilized) rats of LSD (1) (15 or 150 µg/kg, i.v.) evoked widespread 10–30% reductions in CMRglc, notably throughout neocortex, and in thalamus, lateral geniculate, the basal ganglia, and the raphé nuclei, but with little effect in cerebellum [134].”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [134]
Cites
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SEROTONIN IN THE REGULATION OF BRAIN MICROCIRCULATION
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Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans.
Cumming, P., Scheidegger, M., Dornbierer, D., Palner, M., Quednow, B. B., & Martin-Soelch, C. (2021) · Molecules · doi:10.3390/molecules26092451 · Cited by 43 · see citing works
- Authors
- Grome, J. J., & Harper, A. M.
- Affiliations
- University of Glasgow (GB)
- Corresponding author
- Grome, John J.
- ORCID
- Harper, A. Murray
- Venue
- Journal of Neurochemistry
- Publisher
- Wiley
- Published
- 1986-01
- Volume
- 46
- Issue
- 1
- Pages
- 117-124
- ISSN
- 0022-3042 (ISSN-L)
- 1471-4159
- OpenAlex
- W2058119419
- Cited by
- 39
- References
- 1
- Citations by year
- 2026: 1 · 2025: 2 · 2021: 2
- FWCI
- 1.12
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Neurochemistry (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- lysergic acid diethylamide, 5-MeO-DMT, quipazine, indoleamines, piperazine, diencephalon, nucleus reuniens, caudate nucleus, brain energy metabolism
- MeSH terms
- Animals, Autoradiography, Behavior, Animal, Brain, Deoxyglucose, Glucose, Guinea Pigs, Lysergic Acid Diethylamide, Male, Methoxydimethyltryptamines, Pyrazines, Quinolines, Quipazine, Rats, Inbred Strains, Receptors, Serotonin, Serotonin, Rats
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