Document Detail

The tyramine binding site in the central nervous system: an overview.
MedLine Citation:
PMID:  8396735     Owner:  NLM     Status:  MEDLINE    
The [3H]Tyramine (TY) binding site is proposed as a high affinity marker of the membrane carrier for dopamine (DA) in synaptic vesicles from DA-rich brain regions. Under precise assay conditions, there is neither a consistent association of TY with the neuronal, cocaine-sensitive DA transporter, nor with mitochondrial or microsomal targets. TY-labeled sites have a high affinity for selected toxins such as the Parkinsonian agent MPP+ (1-methyl-4-phenylpyridinium ion), or drugs such as diphenylalkylamine Ca(2+)-channel antagonists. The MPP+/TY site interaction, which in the striatum leads to depletion of vesicular DA, occurs in dopaminergic as well as in noradrenergic regions, though with different kinetic profiles. TY-labeled carriers for DA and noradrenaline (NA) in respective vesicles seem to be different entities, which might result in a region-specific rate of toxin sequestration and/or release from heterogeneous vesicles. Whereas MPP+ is a potent competitive-type inhibitor of [3H]TY binding, prenylamine-like Ca(2+)-channel antagonists can compete with TY for the vesicle site, in a tetrabenazine- or reserpine-like manner, and also inhibit TY binding thanks to the extra-channel directed impairment of membrane bioenergetics they are proposed to provoke. This follows from the generally-accepted assumption that similar mechanisms are operational for secretory organelles in adrenals and CNS, and from the marked sensitivity of TY binding to miscellaneous energy-disrupting agents.(ABSTRACT TRUNCATED AT 250 WORDS)
A Vaccari
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Neurochemical research     Volume:  18     ISSN:  0364-3190     ISO Abbreviation:  Neurochem. Res.     Publication Date:  1993 Aug 
Date Detail:
Created Date:  1993-10-08     Completed Date:  1993-10-08     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  7613461     Medline TA:  Neurochem Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  861-8     Citation Subset:  IM    
Department of Neuroscience, B. Brodie, Cagliari, Italy.
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MeSH Terms
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / pharmacology
Binding Sites
Brain / metabolism*
Calcium Channel Blockers / pharmacology
Dopamine / metabolism
Receptors, Biogenic Amine*
Receptors, Neurotransmitter / drug effects,  metabolism*
Tyramine / metabolism*
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Receptors, Biogenic Amine; 0/Receptors, Neurotransmitter; 0/tyramine receptor; 28289-54-5/1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; 51-67-2/Tyramine

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