Effects of WAY 100635 and (-)-5-Me-8-OH-DPAT, a novel 5-HT1A receptor antagonist, on 8-OH-DPAT responses

European Journal of Pharmacology
A C TrillatA M Gardier

Abstract

The neurochemical profile at both post and presynaptic 5-HT1A receptors of a novel 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) analog, 5-methyl-8-hydroxy-2-(di-n-propylamino)tetralin ¿(+/-)-5-Me-8-OH-DPAT¿ and its stereoisomers was determined and compared to that of the highly selective 5-HT1A receptor antagonist, N-[4-(2-methoxyphenyl)-1-piperazinyl]-N-(2-pyridinyl) cyclo-hexanecarboxamide (WAY 100635). We evaluated their effects on 8-OH-DPAT-induced decrease in cAMP production, on 8-OH-DPAT-induced decrease in rat ventral hippocampal extracellular 5-hydroxytryptamine (5-HText) levels and in body temperature in mice. Both (+/-)- and (-)-5-Me-8-OH-DPAT blocked the 8-OH-DPAT-induced inhibition of forskolin-stimulated cAMP production. Moreover, while having no significant effect when injected alone, (+/-)-, (-)-5-Me-8-OH-DPAT and WAY 100635 antagonized the 8-OH-DPAT-induced decrease in 5-HText in rats and hypothermia in mice. By contrast, the (+) isomer inhibited the cAMP synthesis and did not modify the 8-OH-DPAT response on 5-HText in ventral hippocampus. These data suggest that (+/-)-5-Me-8-OH-DPAT acts selectively, its activity residing in the (-) enantiomer, this latter compound acting similarly to WAY 100635 as a ful...Continue Reading

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Citations

Oct 31, 1998·European Journal of Pharmacology·A C TrillatA M Gardier
Dec 8, 2000·Advanced Drug Delivery Reviews·G Boschi, J Scherrmann
Sep 24, 2005·Autonomic & Autacoid Pharmacology·R Villalobos-MolinaI A Gallardo-Ortíz
Feb 22, 2011·Neuropharmacology·Jean-Philippe GuillouxAlain M Gardier
Jun 15, 2007·The International Journal of Neuropsychopharmacology·Bruno P GuiardAlain M Gardier
Sep 19, 2002·Journal of Psychopharmacology·Mei-See ManR Hamish McAllister-Williams
Aug 23, 2003·International Journal of Impotence Research·K FurukawaT Uchiyama

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