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Psychostimulant-like effects of p-fluoroamphetamine in the rat.
Eur J Pharmacol. 1995 Dec 12; 287(2):105-13.EJ

Abstract

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.

Authors+Show Affiliations

Departments of Pharmacology and Toxicology, and Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, IN 47907, USA.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

8749023

Citation

Marona-Lewicka, D, et al. "Psychostimulant-like Effects of P-fluoroamphetamine in the Rat." European Journal of Pharmacology, vol. 287, no. 2, 1995, pp. 105-13.
Marona-Lewicka D, Rhee GS, Sprague JE, et al. Psychostimulant-like effects of p-fluoroamphetamine in the rat. Eur J Pharmacol. 1995;287(2):105-13.
Marona-Lewicka, D., Rhee, G. S., Sprague, J. E., & Nichols, D. E. (1995). Psychostimulant-like effects of p-fluoroamphetamine in the rat. European Journal of Pharmacology, 287(2), 105-13.
Marona-Lewicka D, et al. Psychostimulant-like Effects of P-fluoroamphetamine in the Rat. Eur J Pharmacol. 1995 Dec 12;287(2):105-13. PubMed PMID: 8749023.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Psychostimulant-like effects of p-fluoroamphetamine in the rat. AU - Marona-Lewicka,D, AU - Rhee,G S, AU - Sprague,J E, AU - Nichols,D E, PY - 1995/12/12/pubmed PY - 1995/12/12/medline PY - 1995/12/12/entrez SP - 105 EP - 13 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 287 IS - 2 N2 - 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. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/8749023/Psychostimulant_like_effects_of_p_fluoroamphetamine_in_the_rat_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014-2999(95)00478-5 DB - PRIME DP - Unbound Medicine ER -