The noradrenergic neurotoxins DSP4 and xylamine bind to opiate receptors

DSP4 and xylamine compete with [3H]-naloxone for opiate binding sites with IC50 values of approximately 1 microM. This effect can be blocked by excess naloxone but not by the noradrenaline uptake inhibitors cocaine or desipramine. Other drugs containing the 2-chloroalkylamine structure--phenoxybenza...

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Bibliographic Details
Published inBrain research bulletin Vol. 14; no. 5; p. 493
Main Authors Wilkinson, M, Jacobson, W, Wilkinson, D A
Format Journal Article
LanguageEnglish
Published United States 01.01.1985
Subjects
Amines - metabolism
Animals
Benzylamines - metabolism
Binding, Competitive
Cerebral Cortex - metabolism
Cocaine - pharmacology
Desipramine - pharmacology
Female
In Vitro Techniques
Male
Naloxone - metabolism
Nitrogen Mustard Compounds - metabolism
Rats
Rats, Inbred Strains
Receptors, Opioid - metabolism
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Summary:DSP4 and xylamine compete with [3H]-naloxone for opiate binding sites with IC50 values of approximately 1 microM. This effect can be blocked by excess naloxone but not by the noradrenaline uptake inhibitors cocaine or desipramine. Other drugs containing the 2-chloroalkylamine structure--phenoxybenzamine, dibenamine, chloroethyl clonidine, the cholinotoxin AF-64 and 2-dimethylaminoethyl chloride--were similarly tested. Phenoxybenzamine and dibenamine were also able to compete with [3H]-naloxone for binding at the opiate receptor. Experiments in vivo demonstrated that DSP4, like other opiates, can rapidly reduce LH secretion in the rat. This effect is prevented by naloxone but not by desipramine. These data suggest the use of caution in interpreting the results of experiments in which DSP4 and xylamine are used as "specific" noradrenergic uptake inhibitors or as neurotoxins.
ISSN:0361-9230
DOI:10.1016/0361-9230(85)90028-0