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Titolo:
CLOZAPINE AND N-DESMETHYLCLOZAPINE ARE POTENT 5-HT(1C) RECEPTOR ANTAGONISTS
Autore:
KUOPPAMAKI M; SYVALAHTI E; HIETALA J;
Indirizzi:
UNIV TURKU,DEPT PHARMACOL,KIINAMYLLYNKATU 10 SF-20520 TURKU 52 FINLAND
Titolo Testata:
European journal of pharmacology. Molecular pharmacology section
fascicolo: 2, volume: 245, anno: 1993,
pagine: 179 - 182
SICI:
0922-4106(1993)245:2<179:CANAP5>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
BINDING; SITES; BRAIN;
Keywords:
CLOZAPINE; N-DESMETHYLCLOZAPINE; CLOZAPINE N-OXIDE; 5-HT(1C) RECEPTORS; CHOROID PLEXUS;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
14
Recensione:
Indirizzi per estratti:
Citazione:
M. Kuoppamaki et al., "CLOZAPINE AND N-DESMETHYLCLOZAPINE ARE POTENT 5-HT(1C) RECEPTOR ANTAGONISTS", European journal of pharmacology. Molecular pharmacology section, 245(2), 1993, pp. 179-182

Abstract

The effects of the atypical antipsychotic drug, clozapine, and its two major metabolites in man, N-desmethylclozapine and clozapine N-oxide, on 5-HT1C receptor mediated phosphoinositide hydrolysis were studiedin rat choroid plexus. Clozapine and N-desmethylclozapine antagonized5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 110 and 29.4 nM, respectively. Clozapine N-oxide was less potent. None of the compounds stimulated phosphoinositide hydrolysis per se. The K(i) values for [H-3]mesulergine displacement in choroid plexus were in accordance with phosphoinositide hydrolysis data. In conclusion, this study demonstrates that clozapine and one of its major metabolites in man,N-desmethylclozapine, are potent 5-HT1C receptor antagonists. These properties of clozapine and N-desmethylclozapine should be considered when the atypical effects of clozapine are evaluated in vivo.

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Documento generato il 17/01/20 alle ore 20:22:53