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Titolo:
Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1 alpha metabotropic glutamate receptor
Autore:
Hermans, E; Nahorski, SR; Challiss, RAJ;
Indirizzi:
Univglandester, Dept Cell Physiol & Pharmacol, Leicester LE1 9HN, Leics, En Univ Leicester Leicester Leics England LE1 9HN icester LE1 9HN, Leics, En
Titolo Testata:
NEUROPHARMACOLOGY
fascicolo: 12, volume: 37, anno: 1998,
pagine: 1645 - 1647
SICI:
0028-3908(199812)37:12<1645:RANAPO>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Keywords:
glutamate; mGlu1 alpha receptor; phosphoinositide hydrolysis; non-competitive antagonist; CPCCOEt;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
11
Recensione:
Indirizzi per estratti:
Indirizzo: Hermans, E Univ Catholique Louvain, Pharmacol Lab, UCL 54-10,Ave Hippocrate 54, B-1200 Univ Catholique Louvain UCL 54-10,Ave Hippocrate 54 Brussels Belgium B-1200
Citazione:
E. Hermans et al., "Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1 alpha metabotropic glutamate receptor", NEUROPHARM, 37(12), 1998, pp. 1645-1647

Abstract

In transfected CHO cells expressing the human metabotropic glutamate receptor mGlu1 alpha, 7- hydroxyimino)cyclopropan[b]chromen-1a-carboxylic acid ethylester (CPCCOEt) was found to antagonize L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner (apparent pK(i) value, 4.76 +/- 0.18: It = 3. This suggests that CPCCOEt antagonizes type Ir metabotropic glutamate receptor activation by interacting with a site distinct from the agonist binding site. (C) 1998 Elsevier Science Ltd. All rights reserved.

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Documento generato il 27/09/20 alle ore 00:52:39