Document Detail

Studies on the melanin affinity of selegiline (deprenyl) and other amphetamine derivatives.
MedLine Citation:
PMID:  3124086     Owner:  NLM     Status:  MEDLINE    
The main aim of our study was to assess the melanin affinity of selegiline as well as the pharmacologic and pharmacokinetic aspects of its binding. The in vivo melanin binding of [14C] selegiline was studied by the method of whole body autoradiography. Extensive accumulation was observed in the pigmented mouse eye while in the albino animal uptake was low in the corresponding tissues. Our in vitro investigations demonstrated that the amphetamine derivatives tested can be taken up by melanins. Scatchard analysis of selegiline binding to the dopamine melanin (structurally similar to the neuromelanin) and beef eye melanin showed that more than one class of binding sites may be implicated. The total binding capacity of the beef-eye melanin was higher than that of the dopamine melanin. The selegiline inhibition of the [3H] MPP+ (the neurotoxic metabolite of MPTP) binding to dopamine melanin was also investigated. In the studied concentration range, the binding of [3H] MPP+ was depressed to about 70 per cent of the original maximum value. In conclusion, as a result of its melanin affinity, which is demonstrated in this study, selegiline may most probably accumulate in the pigmented nerve cells. The observed melanin affinity may contribute to the application of this compound for the treatment of Parkinson's disease or may play a role in its protective effect against MPTP neurotoxicity.
G Báthory; T Szüts; K Magyar
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Polish journal of pharmacology and pharmacy     Volume:  39     ISSN:  0301-0244     ISO Abbreviation:  Pol J Pharmacol Pharm     Publication Date:    1987 Mar-Apr
Date Detail:
Created Date:  1988-03-08     Completed Date:  1988-03-08     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  0366561     Medline TA:  Pol J Pharmacol Pharm     Country:  POLAND    
Other Details:
Languages:  eng     Pagination:  195-201     Citation Subset:  IM    
Department of Pharmacodynamics, Semmelweis Medical School, Budapest, Hungary.
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MeSH Terms
Amphetamine / pharmacology*
Binding, Competitive / drug effects
Melanins / metabolism*
Mice, Inbred C57BL
Phenethylamines / pharmacokinetics*
Pyridinium Compounds / metabolism
Receptors, Dopamine / drug effects,  metabolism
Selegiline / pharmacokinetics*
Reg. No./Substance:
0/Melanins; 0/Phenethylamines; 0/Pyridinium Compounds; 0/Receptors, Dopamine; 14611-51-9/Selegiline; 300-62-9/Amphetamine; 42850-10-2/1-(4-methoxyphenyl)pyridinium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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