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5-HT1A receptor-mediated G protein activation assessed by [35S]GTPgammaS binding in rat cerebral cortex.
Eur J Pharmacol. 2005 Oct 03; 521(1-3):49-58.EJ

Abstract

To date, 5-hydroxytryptamine1A (5-HT1A) receptor-mediated functional assays (adenylyl cyclase inhibition, high-affinity GTPase activity and [35S]guanosine-5'-O-(gamma-thio)-triphosphate ([35S]GTPgammaS) binding) have been performed mainly in hippocampal membranes. In the current study, 5-HT-stimulated G protein activation assays were carried out in rat cerebral cortical membranes. High-affinity GTPase activity was stimulated by 5-HT, but not by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). By contrast, 5-HT- and 8-OH-DPAT-stimulated [35S]GTPgammaS binding displayed sufficient dynamic range enough to warrant further pharmacological analysis. Under standard conditions, which were determined precisely in terms of the concentrations of GDP, MgCl2 and NaCl, the profile of 5-HT-stimulated [35S]GTPgammaS binding investigated using a series of 5-HT receptor agonists and antagonists clearly indicated the involvement of the 5-HT1A receptor subtype. There appeared to be no evidence supporting the presence of regional heterogeneity in coupling efficiency between 5-HT1A and G proteins in the hippocampus or cortex. This method is a useful tool for investigating functional coupling between postsynaptic 5-HT1A receptors and G proteins in cerebral cortical membranes.

Authors+Show Affiliations

Department of Psychiatry, Saitama Medical School, 38 Morohongo, Moroyama-machi, Iruma-gun, Staitama 350-0495, Japan. odagaki@saitama-med.ac.jpNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16182280

Citation

Odagaki, Yuji, and Ryoichi Toyoshima. "5-HT1A Receptor-mediated G Protein Activation Assessed By [35S]GTPgammaS Binding in Rat Cerebral Cortex." European Journal of Pharmacology, vol. 521, no. 1-3, 2005, pp. 49-58.
Odagaki Y, Toyoshima R. 5-HT1A receptor-mediated G protein activation assessed by [35S]GTPgammaS binding in rat cerebral cortex. Eur J Pharmacol. 2005;521(1-3):49-58.
Odagaki, Y., & Toyoshima, R. (2005). 5-HT1A receptor-mediated G protein activation assessed by [35S]GTPgammaS binding in rat cerebral cortex. European Journal of Pharmacology, 521(1-3), 49-58.
Odagaki Y, Toyoshima R. 5-HT1A Receptor-mediated G Protein Activation Assessed By [35S]GTPgammaS Binding in Rat Cerebral Cortex. Eur J Pharmacol. 2005 Oct 3;521(1-3):49-58. PubMed PMID: 16182280.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 5-HT1A receptor-mediated G protein activation assessed by [35S]GTPgammaS binding in rat cerebral cortex. AU - Odagaki,Yuji, AU - Toyoshima,Ryoichi, Y1 - 2005/09/21/ PY - 2005/07/12/received PY - 2005/07/19/accepted PY - 2005/9/27/pubmed PY - 2006/1/26/medline PY - 2005/9/27/entrez SP - 49 EP - 58 JF - European journal of pharmacology JO - Eur. J. Pharmacol. VL - 521 IS - 1-3 N2 - To date, 5-hydroxytryptamine1A (5-HT1A) receptor-mediated functional assays (adenylyl cyclase inhibition, high-affinity GTPase activity and [35S]guanosine-5'-O-(gamma-thio)-triphosphate ([35S]GTPgammaS) binding) have been performed mainly in hippocampal membranes. In the current study, 5-HT-stimulated G protein activation assays were carried out in rat cerebral cortical membranes. High-affinity GTPase activity was stimulated by 5-HT, but not by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). By contrast, 5-HT- and 8-OH-DPAT-stimulated [35S]GTPgammaS binding displayed sufficient dynamic range enough to warrant further pharmacological analysis. Under standard conditions, which were determined precisely in terms of the concentrations of GDP, MgCl2 and NaCl, the profile of 5-HT-stimulated [35S]GTPgammaS binding investigated using a series of 5-HT receptor agonists and antagonists clearly indicated the involvement of the 5-HT1A receptor subtype. There appeared to be no evidence supporting the presence of regional heterogeneity in coupling efficiency between 5-HT1A and G proteins in the hippocampus or cortex. This method is a useful tool for investigating functional coupling between postsynaptic 5-HT1A receptors and G proteins in cerebral cortical membranes. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/16182280/5_HT1A_receptor_mediated_G_protein_activation_assessed_by_[35S]GTPgammaS_binding_in_rat_cerebral_cortex_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(05)00751-X DB - PRIME DP - Unbound Medicine ER -