Ring-substituted amphetamine interactions with neurotransmitter receptor binding sites in human cortex.
Pamela A. Pierce, Stephen J. Peroutka
Neuroscience Letters December 19, 1988 DOI: 10.1016/0304-3940(88)90658-1 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro binding affinity study Peer reviewed |
|---|---|
| Population | Human cortex tissue |
| Interventions | MDA MDE MDMA |
| Key points | MDA, MDE, and MDMA all bound with highest affinity (approximately 1 microM) to the 'DOB binding site' labeled by [77Br]R(-)DOB in human cortex. MDA also showed moderate affinity (4-5 microM) at 5-HT1A, 5-HT1D, and alpha 2-adrenergic sites, whereas MDE and MDMA had lower affinity or were inactive at all other sites tested. |
Abstract
The binding affinities of 3 ring-substituted amphetamine compounds were determined at 9 neurotransmitter binding sites in human cortex. (+/-)-3,4-Methylenedioxyamphetamine (MDA), (+/-)-3,4-methylenedioxyethamphetamine (MDE), and (+/-)-3,4-methylenedioxymethamphetamine (MDMA or 'Ecstasy') all display highest affinity (approximately 1 microM) for the recently identified 'DOB binding site' labeled by [77Br]R(-)4-bromo-2,5-dimethoxyphenylisopropylamine [( 77Br]R(-)DOB). MDA displays moderate affinity (4-5 microM) for the 5-hydroxytryptamine1A (5-HT1A), 5-HT1D, and alpha 2-adrenergic sites in human cortex. MDE and MDMA display lower affinity or are inactive at all other sites tested in the present study. These observations are discussed in relation to the novel psychoactive effects of the ring-substituted amphetamines.
Citations in the library
Cited by 4
- The Neuropsychopharmacology and Toxicology of 3,4‐methylenedioxy‐N‐ethyl‐amphetamine (MDEA) CNS Drug Reviews June 1, 2004
- The health effects of ecstasy: a literature review. Drug and Alcohol Review March 2002
- Effects of MDA on classical conditioning of the rabbit nictitating membrane response. Pharmacology, Biochemistry, and Behavior May 1991
- 3,4-Methylenedioxyamphetamine (MDA) analogues exhibit differential effects on synaptosomal release of 3H-dopamine and 3H-5-hydroxytryptamine. Pharmacology, Biochemistry, and Behavior March 1991
Cites 10
- 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. Journal of Pharmacology and Experimental Therapeutics September 1, 1987
- Subjective Reports of the Effects of MDMA in a Clinical Setting Journal of Psychoactive Drugs October 1, 1986
- Hallucinogenic Amphetamine Selectively Destroys Brain Serotonin Nerve Terminals Science September 6, 1985
- The Background and Chemistry of MDMA Journal of Psychoactive Drugs October 1, 1986
- Multiple Severe Complications From Recreational Ingestion of MDMA ('Ecstasy') JAMA August 14, 1987
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