Neurotensin modulates central muscarinic receptors, an effect which does not involve the high-affinity neurotensin receptor (NTS1)
Autor: | G. Rodríguez de Lores Arnaiz, Patricia G. Schneider, M.G. López Ordieres |
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Rok vydání: | 2010 |
Předmět: |
Male
medicine.medical_specialty Physiology Otras Ciencias Biológicas Clinical Biochemistry Neuropeptide Biochemistry SR 48692 Ciencias Biológicas Cellular and Molecular Neuroscience chemistry.chemical_compound Endocrinology Internal medicine Muscarinic acetylcholine receptor medicine Animals Receptors Neurotensin CNS MEMBRANES Neurotensin receptor Rats Wistar Neurotransmitter Receptor Neurotensin Acetylcholine receptor Antagonist Receptors Muscarinic Molecular biology Rats chemistry NEUROTENSINERGIC SYSTEM CHOLINERGIC MUSCARINIC RECEPTOR CIENCIAS NATURALES Y EXACTAS |
Zdroj: | Regulatory Peptides. 163:37-42 |
ISSN: | 0167-0115 |
DOI: | 10.1016/j.regpep.2010.04.002 |
Popis: | Neurotensin (NT) is a tridecapeptide distributed in central and peripheral nervous systems, which can behave as a neurotransmitter or neuromodulator at central and peripheral levels. Herein we tested the potential effect of this peptide on quinuclidinyl benzilate ([3H]-QNB) binding to muscarinic receptor in rat CNS membranes. It was observed that NT decreased up to 50-70% ligand binding at 1×10-7M-1×10-5M concentration in cerebral cortex, cerebellum and striatum. In the hippocampus, NT exerted a biphasic effect, behaving as a stimulator in the presence of 1×10-12M-1×10-10M concentration but as an inhibitor at 1×10-8M-1×10-5M concentration. In order to test the involvement of high-affinity NT receptor (NTS1) in NT inhibitory effect, assays were carried out in the presence of 1×10-6M NT and/or SR 48692 (Sanofi-Aventis, U.S., Inc.), a specific antagonist for this receptor, dissolved in dimethylsulfoxide (DMSO) 10% v/v. As controls, membranes incubated with DMSO and/or NT 1×10-6M plus DMSO were processed. It was found that NT+DMSO decreased [3H]-QNB binding to cerebral cortex, cerebellum and hippocampal membranes by 49%, 32% and 53%, respectively. This inhibition was not observed with the DMSO control group. Membrane preincubation with 1×10-6M SR 48692 failed to alter NT effect on binding. SR 48692 at 1×10-6M concentration decreased the binding by 50% only in cerebral cortex membranes, suggesting a possible direct effect of the antagonist on muscarinic receptors in this area. It was therefore concluded that the high-affinity NT receptor may not be involved in ligand binding inhibition to muscarinic receptor by NT. Fil: Schneider, Patricia Graciela. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Biología Celular y Neurociencia "Prof. Eduardo de Robertis". Universidad de Buenos Aires. Facultad de Medicina. Instituto de Biología Celular y Neurociencia; Argentina Fil: López Ordieres, María Graciela. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Biología Celular y Neurociencia "Prof. Eduardo de Robertis". Universidad de Buenos Aires. Facultad de Medicina. Instituto de Biología Celular y Neurociencia; Argentina Fil: Rodriguez, Georgina Emma. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Biología Celular y Neurociencia "Prof. Eduardo de Robertis". Universidad de Buenos Aires. Facultad de Medicina. Instituto de Biología Celular y Neurociencia; Argentina |
Databáze: | OpenAIRE |
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