The role of 5-HT(1B/1D) receptors in the modulation of 5-hydroxytryptamine levels in the frontal cortex of the conscious guinea pig

European Journal of Pharmacology
C RobertsB J Jones

Abstract

The role of 5-HT(1B/1D) receptors in modulating extracellular 5-hydroxytryptamine (5-HT) levels in the guinea pig was investigated with the non-selective 5-HT(1B/1D) receptor inverse agonist, methiothepin, and the selective 5-HT(1B/1D) receptor partial agonists, GR 127935 (n-[4-methoxy-3-(4-methyl-1-piperizinyl)phenyl]-2'-methyl-4'-(5-me thyl-1,2,4-oxadiazole-3-yl)[1,1'-biphenyl]-4-carboxamide) and GR 125743 (n-[4-methoxy-3-(4-methyl-1-piperizinyl)phenyl]-3-methyl-4-(4-pyri dinyl)benzamide). Extracellular 5-HT levels were measured using the technique of brain microdialysis, in the frontal cortex of the freely moving guinea-pig. Extracellular 5-HT was tetrodotoxin sensitive and calcium dependent, and increased when perfused with a high concentration of K+. In addition, extracellular 5-HT levels were lowered by the 5-HT(1B/1D) receptor agonist, sumatriptan, and the 5-HT1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin, while perfusion of the selective serotonin re-uptake inhibitor, paroxetine, increased 5-HT in a concentration-dependent manner. Perfusion of methiothepin, GR 127935 and GR 125743 into the frontal cortex caused significant but transient increases of extracellular 5-HT. However, systemic administration of m...Continue Reading

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Citations

Mar 28, 2008·Journal of Comparative Physiology. A, Neuroethology, Sensory, Neural, and Behavioral Physiology·María Ana Calviño, Lidia Szczupak
Dec 26, 2001·Brain Research Bulletin·C RobertsD N Middlemiss
Dec 5, 2000·Alcoholism, Clinical and Experimental Research·C H JengY Wang
Feb 3, 1999·Annals of the New York Academy of Sciences·P BlierC de Montigny
Feb 21, 2006·NeuroRx : the Journal of the American Society for Experimental NeuroTherapeutics·Lee E SchechterSharon Rosenzweig-Lipson
Mar 22, 2006·Psychopharmacology·R M M De AlmeidaK A Miczek
Jul 16, 2013·Experimental Lung Research·José Luis Arreola-RamírezPatricia Segura-Medina
Dec 10, 2009·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·P SeguraL M Montaño
Dec 6, 2005·European Journal of Pharmacology·Rosa M M de AlmeidaKlaus A Miczek
Aug 1, 2007·Expert Opinion on Therapeutic Patents·Yiyun Huang, Wendol A Williams
Oct 3, 2008·Bioorganic & Medicinal Chemistry Letters·Halina T SerafinowskaJeannette M Watson
May 17, 2000·AIDS Patient Care and STDs·N J OstropM J Gill
Feb 7, 2002·CNS Drug Reviews·C RobertsD N Middlemiss

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