Document Detail

Psychostimulant-like effects of p-fluoroamphetamine in the rat.
MedLine Citation:
PMID:  8749023     Owner:  NLM     Status:  MEDLINE    
The present study was undertaken to compare the pharmacological properties of p-fluoroamphetamine with those of amphetamine and of other halogenated amphetamines, using several in vivo and in vitro tests. These included substitution testing in (+)-amphetamine (1 mg/kg, 5.4 mu mol/kg, i.p.)-, (+)-N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine [(+)-MBDB] (1.75 mg/kg, 7.8 mu mol/kg, i.p.)-, and 5-methoxy-6-methyl-2-aminoindan (MMAI) (1.71 mg/kg, 8 mu mol/kg, i.p.)-trained rats, [3H]5-HT and [3H]dopamine uptake inhibition in whole brain synaptosomes, and changes in striatal extracellular levels of dopamine, 3,4-dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) as measured by in vivo microdialysis in freely moving rats. In drug discrimination substitution tests, p-fluoroamphetamine fully mimicked (+)-amphetamine (ED50 0.43 mg/kg, 2.11 mu mol/kg), whereas 'no substitution' was observed in rats trained to discriminate the serotonin (5-hydroxytryptamine, 5-HT)-releasing agents (+)-MBDB or MMAI from saline. p-Chloroamphetamine did not substitute for amphetamine but fully substituted for the (+)-MBDB and MMAI cues (ED50 0.17 mg/kg, 0.82 mu mol/kg, and 0.14 mg/kg, 0.69 mu mol/kg, respectively). p-Fluoroamphetamine, in comparison with p-chloroamphetamine and p-iodoamphetamine, showed much stronger inhibition of [3H]dopamine than [3H]5-HT uptake into rat brain synaptosomes but was less selective than amphetamine. p-Fluoroamphetamine (7.0 mg/kg, i.p.), 1 h after administration, strongly elevated (849% of baseline) extracellular dopamine in rat striatum measured using in vivo microdialysis. Amphetamine (2 mg/kg, i.p.) increased extracellular dopamine in rat striatum with a maximum at the same time as did p-fluoroamphetamine, but the latter gave a smaller increase. The data presented suggest that p-fluoroamphetamine resembles amphetamie more than it does the 5-HT-releasing type amphetamines.
D Marona-Lewicka; G S Rhee; J E Sprague; D E Nichols
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  European journal of pharmacology     Volume:  287     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1995 Dec 
Date Detail:
Created Date:  1996-10-24     Completed Date:  1996-10-24     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  105-13     Citation Subset:  IM    
Departments of Pharmacology and Toxicology, and Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, IN 47907, USA.
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MeSH Terms
3,4-Dihydroxyphenylacetic Acid / metabolism
3,4-Methylenedioxyamphetamine / analogs & derivatives,  pharmacology
Amphetamine / pharmacology*
Amphetamines / pharmacology*
Behavior, Animal / drug effects
Discrimination (Psychology) / drug effects
Dose-Response Relationship, Drug
Rats, Sprague-Dawley
Time Factors
Reg. No./Substance:
0/Amphetamines; 102-32-9/3,4-Dihydroxyphenylacetic Acid; 103818-46-8/N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine; 300-62-9/Amphetamine; 459-02-9/4-fluoroamphetamine; 4764-17-4/3,4-Methylenedioxyamphetamine

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