The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons

European Journal of Pharmacology
J MosB Olivier

Abstract

Twelve homing pigeons were trained to discriminate the 5-HT1A receptor agonist flesinoxan (0.25 mg/kg p.o.) from its vehicle in a fixed ratio (FR) 30 two-key operant drug discrimination procedure. Tests for generalization and antagonism showed that compounds with agonistic action at the 5-HT1A receptor, such as 8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), buspirone and ipsapirone all substituted for the flesinoxan cue. Compounds with mixed agonistic action at the 5-HT(1A/1B) receptor fully (eltoprazine) or partially (RU24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl-1H-indole)) substituted for flesinoxan. TFMPP (1-(3-trifluoromethylphenyl)piperazine) and mCPP (1-(3-chlorophenyl)piperazine), both acting at the 5-HT(1B/2C) receptor, did not substitute for flesinoxan, neither did the selective 5-HT re-uptake inhibitor fluvoxamine. The results of the antagonism tests showed that the 5-HT1A receptor antagonists NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine), WAY 100635 ((N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclo-he xane-carboxamide) and the newly developed DU125530 (2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl ]butyl]-1,2-benzisothiazol-3(2H)-one-1,1-dioxid...Continue Reading

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Citations

Oct 27, 1998·European Journal of Pharmacology·J De Vry, K R Jentzsch
Dec 14, 2002·Pharmacology, Biochemistry, and Behavior·F MirandaD N Velázquez-Martínez
Oct 9, 1999·Pharmacology, Biochemistry, and Behavior·B OlivierT Hijzen
Jan 12, 1999·Neuroscience and Biobehavioral Reviews·B OlivierK A Miczek
Jul 28, 1999·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·H H Berendsen, C L Broekkamp
Oct 5, 2011·Pharmacology, Biochemistry, and Behavior·Kathleen E Morrison, Matthew A Cooper
Apr 2, 2002·Expert Opinion on Investigational Drugs·Martyn D WoodJeannette M Watson
Mar 30, 2001·Journal of Psychopharmacology·H Sánchez, D N Velázquez-Martínez
Aug 28, 2004·CNS Drugs·Fokko J BoskerJakob Korf

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