G-protein activation at 5-HT1A receptors by the 5-ht1F ligand LY334370 in guinea-pig brain sections and recombinant cell lines

British Journal of Pharmacology
D S DupuisP J Pauwels

Abstract

1. G-protein activation by the 5-ht1F receptor agonist 5-(4-fluorobenzoyl)amino-3-(1-methylpiperidin-4-yl)-1H-indole fumarate (LY334370) was investigated by use of autoradiography of receptor-activated G-proteins in guinea-pig brain sections and [35S]-GTPgammaS binding responses in cell lines stably expressing human 5-HT1A (h 5-HT1A) receptors. 2. LY334370 (10 microM) caused little or no stimulation of [35S]-GTPgammaS binding in guinea-pig brain regions enriched in 5-ht1F binding sites (e.g., claustrum, caudate/putamen and thalamic nuclei), as identified by labelling with 10 nM [3H]-sumatriptan plus 10 nM 5-carboxamidotryptamine (5-CT). 3. Application of LY334370 (10 microM) to guinea-pig brain sections resulted in an increase of [35S]-GTPgammaS binding in hippocampus (123+/-17%), lateral septum (58+/-14%), dorsal raphe (57+/-10%), entorhinal (37+/-11%) and cingulate cortex (28+/-10%). This distribution fits with the G-protein activation mediated by 5-HT1A receptors as found with lisuride (10 microM), and labelling of 5-HT1A receptors by 140 pM [125I]-4-(2'-methoxy-phenyl)- -[2'-(n-2"-pyridinyl)-p-iodobenzamido]-ethyl-piperazine (p-MPPI). 4. The LY334370-mediated [35S]-GTPgammaS response was antagonized by the selective, silent...Continue Reading

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Citations

May 19, 2005·Naunyn-Schmiedeberg's Archives of Pharmacology·David B WainscottDavid L Nelson
Oct 21, 2006·Journal of Computer-aided Molecular Design·Farhad SoltanshahiRobert D Clark
Nov 18, 2004·Bioorganic & Medicinal Chemistry Letters·Deyi ZhangYao-Chang Xu
Sep 27, 2003·Cephalalgia : an International Journal of Headache·N M RamadanK W Johnson
Apr 9, 2005·The Journal of Eukaryotic Microbiology·Parke A RubleeMichael M Marshall
May 13, 2005·Journal of Pharmacological Sciences·Yuji Odagaki, Ryoichi Toyoshima

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