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Titolo:
Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site
Autore:
Knoflach, F; Mutel, V; Kew, JNC; Malherbe, P; Vieira, E; Wichmann, J; Kemp, JA;
Indirizzi:
F Hoffmann La Roche & Co Ltd, Preclin Cent Nervous Syst Res, Div Pharma, CH-4070 Basel, Switzerland F Hoffmann La Roche & Co Ltd Basel Switzerland CH-4070 asel, Switzerland
Titolo Testata:
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
fascicolo: 23, volume: 98, anno: 2001,
pagine: 13402 - 13407
SICI:
0027-8424(20011106)98:23<13402:PAMOMG>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT CEREBELLAR SLICES; SYNAPTIC TRANSMISSION; CALCIUM CHANNELS; TERMINAL DOMAIN; PLASTICITY; ACTIVATION; ANTAGONIST; INHIBITION; PATHWAY; LIGANDS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Mutel, V F Hoffmann La Roche & Co Ltd, Preclin Cent Nervous Syst Res, Div Pharma, PRBN P 70-326, CH-4070 Basel, Switzerland F Hoffmann La Roche & Co Ltd PRBN P 70-326 Basel Switzerland CH-4070
Citazione:
F. Knoflach et al., "Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site", P NAS US, 98(23), 2001, pp. 13402-13407

Abstract

We have identified two chemical series of compounds acting as selective positive allosteric modulators (enhancers) of native and recombinant metabotropic glutamate 1 (mGlu1) receptors. These compounds did not directly activate mGlu1 receptors but markedly potentiated agonist-stimulated responses, increasing potency and maximum efficacy. Binding of these compounds increased the affinity of a radiolabeled glutamate-site agonist at its extracellular N-terminal binding site. Chimeric and mutated receptors were used to localize amino acids in the receptor transmembrane region critical for these enhancing properties. Finally, the compounds potentiated synaptically evoked ri receptor responses in rat brain slices. The discovery of selective positive allosteric modulators of mGlu1 receptors opens up the possibility to develop a similar class of compounds for other family 3 G protein-coupled receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/03/20 alle ore 00:54:17