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[3H]WIN 35,428 binding in the human brain
P Allard1, J O Marcusson, S B Ross
1Department of Psychiatry, University of Umeå, Sweden.
Brain Research
|January 15, 1996
Summary
Researchers investigated [3H]WIN 35,428 binding in human brain regions. Dopamine blocked binding in the putamen, while paroxetine showed similar affinity to cocaine, highlighting cocaine-sensitive sites in the frontal cortex.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- The neurotransmitter dopamine plays a crucial role in brain function.
- Understanding dopamine transporter (DAT) binding is vital for neurological research.
- WIN 35,428 is a radioligand used to study DAT binding sites.
Purpose of the Study:
- To characterize the binding of [3H]WIN 35,428 in post-mortem human brain tissue.
- To investigate the pharmacological profile of these binding sites, particularly in extrastriatal regions.
- To identify the nature of cocaine-sensitive binding sites in the frontal cortex.
Main Methods:
- Radioligand binding assays using [3H]WIN 35,428 on post-mortem human brain sections.
- Competition binding experiments with dopamine and paroxetine.
- Analysis of binding site characteristics, including protein sensitivity.
Main Results:
- Dopamine significantly inhibited [3H]WIN 35,428 binding in the putamen.
- Paroxetine demonstrated comparable affinity to cocaine (200-300 nM) in inhibiting binding.
- [3H]WIN 35,428 labeled protein-nature binding sites sensitive to cocaine and alaproclate in the frontal cortex.
Conclusions:
- The study confirms dopamine's inhibitory effect on [3H]WIN 35,428 binding in the putamen.
- Paroxetine's affinity suggests its potential as a tool for studying DAT.
- Further research is warranted to fully elucidate the cocaine-sensitive binding sites in the frontal cortex.