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Titolo:
Autoradiography of receptor-activated G-proteins in post mortem human brain
Autore:
Rodriguez-Puertas, R; Gonzalez-Maeso, J; Meana, JJ; Pazos, A;
Indirizzi:
Univ Basque Country, Dept Pharmacol, Leioa, Bizkaia, Spain Univ Basque Country Leioa Bizkaia Spain Pharmacol, Leioa, Bizkaia, Spain Univ Cantabria, Fac Med, Pharmacol Unit, Dept Physiol & Pharmacol, Santander 39011, Spain Univ Cantabria Santander Spain 39011 & Pharmacol, Santander 39011, Spain
Titolo Testata:
NEUROSCIENCE
fascicolo: 1, volume: 96, anno: 2000,
pagine: 169 - 180
SICI:
0306-4522(2000)96:1<169:AORGIP>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
GAMMA-S BINDING; MU-OPIOID RECEPTOR; IN-SITU HYBRIDIZATION; ADULT BASAL GANGLIA; CANNABINOID RECEPTOR; RAT-BRAIN; ALPHA-2-ADRENERGIC RECEPTOR; REGIONAL DISTRIBUTION; ALZHEIMERS-DISEASE; FUNCTIONAL RECONSTITUTION;
Keywords:
[S-35]GTP gamma S binding; alpha(2)-adrenoceptors; 5-HT1 receptors; mu-opioid receptors; cholinergic muscarinic receptors; cannabinoid receptors;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
65
Recensione:
Indirizzi per estratti:
Indirizzo: Rodriguez-Puertas, R Univ Basque Country, Dept Pharmacol, Leioa, Bizkaia, Spain Univ Basque Country Leioa Bizkaia Spain kaia, Spain
Citazione:
R. Rodriguez-Puertas et al., "Autoradiography of receptor-activated G-proteins in post mortem human brain", NEUROSCIENC, 96(1), 2000, pp. 169-180

Abstract

The agonist-stimulated guanosine 5'-(gamma-[S-35]thio)triphosphate bindingassay was used to anatomically localize receptor-activated G-proteins by autoradiography in post mortem human brain. The optimal conditions for guanosine 5'-(gamma-S-35]thio)triphosphate binding to human brain sections were established in post mortem samples of the prefrontal cortex, hippocampus, basal ganglia, brainstem and cerebellar cortex. An excess of GDP (2 mM) was required to decrease basal activity and obtain effective stimulation by specific agonists. guanosine 5'-(gamma-[S-35]Thio)triphosphate binding was increased after stimulation with specific agonists of different G-protein-coupled receptors. They include cannabinoid (WIN55212-2), mu-opioid ([D-Ala(2)N-MePh4,Gly(5)-ol]enkephalin), serotonin-1A [(+/-)-8-hydroxy-2-(di-n-propylamino)tetralin and serotonin-1B/1D (sumatriptan), cholinergic muscarinic receptors (carbachol) and alpha(2)-adrenoceptors (UK14304). Such stimulation reached 1458%, 440%, 188%, 219%, 61% and 339%, respectively, over the basal levels. In tissue sections, the use of the above-mentioned agonists (10(-4)M) showed patterns of anatomical distribution similar to those already described by receptor autoradiography, with high densities over the hippocampus (serotonin-1A receptors), cortex (alpha(2)-adrenoceptors) and striatum (mu-opioid receptors). The highest binding levels were reached with the cannabinoid receptor agonist in most of the analysed brain regions. Carbachol produced only moderate stimulation of those same regions. The blockage of agonist-stimulated guanosine 5'-(mu-[S-35]thio)triphosphate binding by selective antagonists verified that the effect was receptor mediated. This technique provides a method to identify modifications of the receptor-mediated activation of G-proteins in post mortem human brain with anatomical resolution. It also provides valuable information on the level of drug efficacy in the human species. (C) 2000 IBRO. Published by Elsevier Science Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 14:32:37