Imaging Brain Phospholipase A2 Activation in Awake Rats in Response to the 5-HT2A/2C Agonist (±)2,5-Dimethoxy-4-Iodophenyl-2-Aminopropane (DOI)
Y. Qu, Lisa Chang, J. Klaff, A. Balbo, S. Rapoport
Neuropsychopharmacology February 1, 2003 DOI: 10.1038/sj.npp.1300022 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Unanesthetized adult rats |
| Interventions | DOI mianserin |
| Dose | 2.5 mg/kg i.p. DOI |
| Topics | Serotonin |
| Key findings | DOI at 2.5 mg/kg i.p. produced widespread increases of about 60% in arachidonic acid incorporation coefficient in neocortical brain regions, which were entirely blocked by chronic mianserin pretreatment. |
Abstract
Incorporation coefficients k* of intravenously injected [3H]arachidonic acid from blood into brain reflect the release from phospholipids of arachidonic acid by receptor-initiated activation of phospholipase A2 (PLA2). In unanesthetized adult rats, 2.5 mg/kg intraperitoneally (i.p.) (±)2,5-dimethoxy-4-iodophenyl-2-aminopropane (DOI), which is a 5-HT2A/2C receptor agonist, has been reported to produce the behavioral changes of what is known as the 5-HT2 syndrome, but only a few small regional decrements in brain glucose metabolism. In this study, 2.5 mg/kg i.p. DOI, when administered to unanesthetized rats, produced widespread and significant increases, of the order of 60%, in k* for arachidonate, particularly in neocortical brain regions reported to have high densities of 5-HT2A receptors. The increases could be entirely blocked by chronic pretreatment with mianserin, a 5-HT2 receptor antagonist. The results suggest that the 5-HT2 syndrome involves widespread brain activation of PLA2 via 5-HT2A receptors, leading to the release of the second messenger, arachidonic acid. Chronic mianserin, a 5-HT2 antagonist, prevents this activation.
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| 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain | 1987 | Animal experiment | |
| Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells | 2006 | In vitro laboratory study |
Citations in the library
Cited by 4
- Psychedelics and Neuroplasticity: A Systematic Review Unraveling the Biological Underpinnings of Psychedelics Frontiers in Psychiatry September 10, 2021
- Hallucinogens. Pharmacology & Therapeutics February 1, 2004
- Could psychedelic drugs have a role in the treatment of schizophrenia? Rationale and strategy for safe implementation. Molecular Psychiatry 2023
- Acute SSRI-induced anxiogenic and brain metabolic effects are attenuated 6 months after initial MDMA-induced depletion. Behavioural Brain Research March 5, 2010
Cites 3
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