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Titolo:
Mixed agonist-antagonist properties of clozapine at different human clonedmuscarinic receptor subtypes expressed in Chinese hamster ovary cells
Autore:
Olianas, MC; Maullu, C; Onali, P;
Indirizzi:
Univlyagliari, Dept Neurosci, Sect Biochem Pharmacol, I-09124 Cagliari, Ita Univ Cagliari Cagliari Italy I-09124 em Pharmacol, I-09124 Cagliari, Ita Univ Cagliari, Dept Med Sci, I-09124 Cagliari, Italy Univ Cagliari Cagliari Italy I-09124 pt Med Sci, I-09124 Cagliari, Italy
Titolo Testata:
NEUROPSYCHOPHARMACOLOGY
fascicolo: 3, volume: 20, anno: 1999,
pagine: 263 - 270
SICI:
0893-133X(199903)20:3<263:MAPOCA>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTRAPYRAMIDAL SYMPTOMS; CHOLINERGIC RECEPTORS; ADENYLYL-CYCLASE; M4 RECEPTOR; CHO CELLS; DRUGS; ACETYLCHOLINE; HALOPERIDOL; DOPAMINE; BINDING;
Keywords:
clozapine; atropine; human muscarinic receptor subtypes; second messengers; receptor binding; [S-35] GTP gamma S binding; Chinese hamster ovary cells;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Onali, P Univ4Cagliari, Dept Neurosci, Sect Biochem Pharmacol, Via Porcell4, I-0912 Univ Cagliari Via Porcell 4 Cagliari Italy I-09124 ell 4, I-0912
Citazione:
M.C. Olianas et al., "Mixed agonist-antagonist properties of clozapine at different human clonedmuscarinic receptor subtypes expressed in Chinese hamster ovary cells", NEUROPSYCH, 20(3), 1999, pp. 263-270

Abstract

We recently reported that clozapine behaves as a partial agonist at the cloned human m4 muscarinic receptor subtype. In the present study, we investigated whether the drug could elicit similar effects at the cloned human m1,m2, and m3 muscarinic receptor subtypes expressed in the Chinese hamster ovary (CHO) cells. Clozapine elicited a concentration-dependent stimulation of [H-3]inositol phosphates accumulation in CHO cells expressing either them1 or the m3 receptor subtype. Moreover, clozapine inhibited forskolin-stimulated cyclic AMP accumulation and enhanced [S-35] GTP gamma S binding to membrane G proteins in CHO cells expressing the m2 receptor. These agonist effects of clozapine were antagonized by atropine. The intrinsic activity of clozapine was lower than that of the full cholinergic agonist carbachol, and, when the compounds were combined, clozapine potently reduced the receptor responses to carbachol. These data indicate that clozapine behaves as apartial agonist at different muscarinic receptor subtypes and may provide ne su hints for understanding the receptor mechanisms underlying the antipsychotic efficacy of the drug. [Neuropsychopharmacology 20:263-270, 1999] (C) 1999 American College of Neuropsychopharmacology. Published by Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 16:14:00