MDMA‐evoked changes in [11C]raclopride and [11C]NMSP binding in living pig brain
Pedro Rosa‐neto, Albert Gjedde, Aage Kristian Olsen Alstrup, Svend Borup Jensen, Ole Lajord Munk, Hideaki Watanabe, Paul Cumming
Synapse July 14, 2004 DOI: 10.1002/syn.20053 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Living pigs |
| Intervention | MDMA |
| Dose | 1 mg/kg, i.v. |
| Duration | 90-minute PET recordings, with scans at 45 and 165 minutes post-infusion |
| Measures | binding potentials of [11C]raclopride and [11C]NMSP |
| Topics | MDMA |
| Keywords | Raclopride Pharmacology |
| Citations | 39 |
| Key findings | MDMA reduced the binding potential of [11C]raclopride and [11C]NMSP to dopamine D2-like receptors in pig striatum, with NMSP binding showing a progressive decline not typically seen with dopamine-releasing drugs. |
Abstract
Abstract Positron emission tomography (PET) studies with radiolabeled dopamine D 2 ‐like receptor ligands reveal d ‐amphetamine‐evoked increases in the competition from endogenous dopamine. However, the corresponding effects of methylenedioxymethamphetamine (MDMA, “Ecstasy”), which releases catecholamines and also serotonin, are unknown. Using PET, we measured the binding potentials ( pB s) of the benzamide [ 11 C]raclopride and the butyrophenone N‐[ 11 C]methylspiperone ([ 11 C]NMSP) in brain of living pigs first in a baseline condition and at 45 and 165 min after infusion of (+/‐)‐MDMA‐HCl (1 mg/kg, i.v.). Concomitant studies of cerebral blood flow did not reveal significant perfusion changes in the cerebellum reference region or in striatum, supporting the present use of reference tissue methods for the mapping of MDMA‐evoked pB changes. Relative to the baseline pB of [ 11 C]raclopride for dopamine D 2/3 receptors in striatum ( pB = 1.5–2.2), MDMA‐treatment reduced pB by 35% in the first posttreatment scan and by 22% in the second posttreatment scan, comparable to changes typically evoked by d ‐amphetamine at a similar dose. In most previous studies, the in vivo binding of butyrophenones has been nearly insensitive to d ‐amphetamine‐evoked dopamine release. However, we found the baseline pB of [ 11 C]NMSP for dopamine D 2 ‐like receptors in striatum ( pB = 4–5) was decreased by 30% in the first post‐MDMA scan and by 50% in the second post‐MDMA scan, irrespective of assumptions about the extent of equilibrium binding attained during the 90‐min‐long PET recordings. Distinct properties of MDMA such as simultaneous release of dopamine and serotonin in brain may account for the present finding of progressive decline in the availability of [ 11 C]NMSP binding sites in striatum. Synapse 53:222–233, 2004. © 2004 Wiley‐Liss, Inc.
Comparable studies
Other experimental studies on MDMA, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| 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 | |
| Oxytocin-dependent reopening of a social reward learning critical period with MDMA | 2019 | Experimental study | |
| Effects of certain hallucinogenic amphetamine analogs on the release of [3H]-serotonin from rat brain synaptosomes Rat whole brain synaptosomes | 1982 | Experimental study |
Citations in the library
Cited by 5
- In Vivo Imaging of Cerebral Serotonin Transporter and Serotonin2A Receptor Binding in 3,4-Methylenedioxymethamphetamine (MDMA or “Ecstasy”) and Hallucinogen Users Archives of General Psychiatry June 6, 2011
- Simultaneous polysubstance use among Danish 3,4‐methylenedioxymethamphetamine and hallucinogen users: combination patterns and proposed biological bases Human Psychopharmacology: Clinical and Experimental June 14, 2012
- A PET study of effects of chronic 3,4‐methylenedioxymethamphetamine (MDMA, “ecstasy”) on serotonin markers in Göttingen minipig brain Synapse April 5, 2007
- Interaction between LSD and dopamine D2/3 binding sites in pig brain Synapse 2005
- Molecular brain imaging of psychedelic action. International review of neurobiology 2025
Cites 9
- Carrier‐Mediated Release of Serotonin by 3,4‐Methylenedioxymethamphetamine: Implications for Serotonin‐Dopamine Interactions Journal of Neurochemistry 1996
- The pharmacology of the acute hyperthermic response that follows administration of 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) to rats British Journal of Pharmacology 2002
- In vivo detection of short- and long-term MDMA neurotoxicity?a positron emission tomography study in the living baboon brain Synapse June 1, 1998
- 3,4-Methylenedioxymethamphetamine (Ecstasy) Inhibits Dyskinesia Expression and Normalizes Motor Activity in 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine-Treated Primates Journal of Neuroscience October 8, 2003
- MDMA: A Review of Epidemiological Data Journal of Psychoactive Drugs June 1, 2002
and 4 more in the library