Research article summary (published 13 Sep 1995):

Discriminative stimulus properties of flesinoxan: effects of enantiomers, (S)-UH301 and WAY-100635.

Full Abstract

Rats were trained to discriminate the specific 5-HT1A receptor agonist (+)-flesinoxan (R(+)-N(-)[2[4-(2,3-dihydro-2-2-hydroxy-methyl-1,4- benzodioxin-5-yl)-1-piperazinyl]ethyl]-4-fluorobenzoamide) (1.5 mg/kg p.o.) from water in a two-lever operant procedure. Generalization tests were conducted with the enantiomers and racemate of flesinoxan and the 5-HT1A receptor antagonists (S)-UH301 ((S)-5-fluoro-8-hydroxy-2-(dipropylamino)-tetralin) and WAY-100635 ((N(-)[2(-)[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride). (S)-UH301, WAY-100635 and fentanyl were investigated for their antagonistic properties. The (+)-flesinoxan stimulus generalized to (-)-flesinoxan and the racemate. The ED50 values for generalization corresponded well with the affinities of the enantiomers and the racemate for the 5-HT1A receptor. The flesinoxan cue could not be mimicked by (S)-UH301 or WAY-100635, but (S)-UH301 reduced response rates. Antagonism tests showed that both (S)-UH301 and WAY-100635 dose dependently antagonized the flesinoxan cue, with ID50 values of 0.52 and 0.03 mg/kg s.c., respectively. Fentanyl had no significant antagonistic properties. It is concluded that rats can learn to discriminate orally administered (+)-flesinoxan from water. The generalization of flesinoxan to the (-)-enantiomer and the antagonism of flesinoxan's cue by specific 5-HT1A receptor antagonists are further evidence for the involvement of flesinoxan's 5-HT1A receptor agonistic properties in its discriminative stimulus effects.

Author information

Author/s: Gommans, J (J); Hijzen, T H (TH); Maes, R A (RA); Mos, J (J); Olivier, B (B);

Affiliation: Department of Psychopharmacology, Faculty of Pharmacy, Utrecht University, Netherlands.

Journal and publication information

Publication Type: Journal Article

Journal: European journal of pharmacology (Eur J Pharmacol), published in NETHERLANDS. (Language: eng)

Reference: 1995-Sep; vol 284 (issue 1-2) : pp 135-40

Dates: Created 1996/02/20; Completed 1996/02/20; Revised 2003/11/14;

PMID: 8549617, status: MEDLINE (last retrieval date: 2/18/2009, IMS Date: )

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

8-Hydroxy-2-(di-n-propylamino)tetralin - administration & dosage; analogs & derivatives; pharmacology Administration, Oral Analgesics, Opioid - pharmacology Animals Discrimination (Psychology) - drug effects Discrimination Learning - drug effects Dose-Response Relationship, Drug Fentanyl - pharmacology Generalization (Psychology) - drug effects

Generalization (Psychology) - drug effects Injections, Subcutaneous Male Piperazines - administration & dosage; antagonists & inhibitors; pharmacology Pyridines - administration & dosage; pharmacology Rats Rats, Wistar Serotonin Antagonists - administration & dosage; pharmacology Stereoisomerism

Associated Chemicals: Analgesics, Opioid (0) ; Piperazines (0) ; Pyridines (0) ; Serotonin Antagonists (0) ; UH 301 (127126-21-0) ; WAY 100635 (146714-97-8) ; Fentanyl (437-38-7) ; 8-Hydroxy-2-(di-n-propylamino)tetralin (78950-78-4) ; flesinoxan (98206-10-1)

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