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Titolo:
Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist
Autore:
Tatarczynska, E; Klodzinska, A; Chojnacka-Wojcik, E; Palucha, A; Gasparini, F; Kuhn, R; Pilc, A;
Indirizzi:
Polish Acad Sci, Inst Pharmacol, PL-31343 Krakow, Poland Polish Acad Sci Krakow Poland PL-31343 harmacol, PL-31343 Krakow, Poland Novartis Pharma AG, Therapeut Area Nervous Syst, Basel, Switzerland Novartis Pharma AG Basel Switzerland a Nervous Syst, Basel, Switzerland Jagiellonian Univ, Collegium Medicum, Inst Publ Hlth, Krakow, Poland Jagiellonian Univ Krakow Poland Medicum, Inst Publ Hlth, Krakow, Poland
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 7, volume: 132, anno: 2001,
pagine: 1423 - 1430
SICI:
0007-1188(200104)132:7<1423:PAAAEO>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
METABOTROPIC GLUTAMATE RECEPTORS; ELEVATED PLUS-MAZE; D-ASPARTATE RECEPTORS; RAT HIPPOCAMPUS; GROUP-I; ANTI-ANXIETY; CA1 REGION; AGONIST; NMDA; SUBTYPES;
Keywords:
mGlu5 receptors; MPEP; conflict drinking test; four-plate test; plus-maze test; tail suspension test; anxiety; depression;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
41
Recensione:
Indirizzi per estratti:
Indirizzo: Pilc, A Polish Acad Sci, Inst Pharmacol, Smetna 12, PL-31343 Krakow, Poland Polish Acad Sci Smetna 12 Krakow Poland PL-31343 3 Krakow, Poland
Citazione:
E. Tatarczynska et al., "Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist", BR J PHARM, 132(7), 2001, pp. 1423-1430

Abstract

1 Several lines of evidence suggest a crucial involvement of glutamate in the mechanism of action of anxiolytic and/or antidepressant drugs. The involvement of group I mGlu receptors in anxiety and depression has also been proposed. Given the recent discovery of a selective and brain penetrable mGlu5 receptor antagonists, the effect of 2-methyl-6-(phenylethynyl)-pyridine (MPEP), i.e, the most potent compound described, was evaluated in established models of anxiety and depression.2 Experiments were performed on male Wistar rats or male Albino Swiss or C57BL/6J mice. The anxiolytic-like effects of MPEP was tested in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. The antidepressant-like effect was estimated using the tail suspension test in mice and the behavioural despair test in rats.3 MPEP (1-30 mg kg(-1)) induced anxioiytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP had no effect on locomotor activity or motor coordination. MPEP (1-20 mg kg(-1)) did shorten the immobility time in a tail suspension test in mice, however it was inactive in the behavioural despair test in rats.4 These data suggest that selective mGlu5 receptor antagonists may play a role in the therapy of anxiety and/or depression, further studies are required to identify the sites and the mechanism of action of MPEP.

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Documento generato il 01/12/20 alle ore 22:46:17