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Titolo:
THE MODERATE AFFINITY OF CLOZAPINE AT H-3 RECEPTORS IS NOT SHARED BY ITS 2 MAJOR METABOLITES AND BY STRUCTURALLY RELATED AND UNRELATED ATYPICAL NEUROLEPTICS
Autore:
SCHLICKER E; MARR I;
Indirizzi:
UNIV BONN,INST PHARMAKOL & TOXIKOL,REUTERSTR 2B D-53113 BONN GERMANY
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 3, volume: 353, anno: 1996,
pagine: 290 - 294
SICI:
0028-1298(1996)353:3<290:TMAOCA>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRAIN CORTEX; BINDING; MOUSE; RAT;
Keywords:
ATYPICAL NEUROLEPTICS; CLOZAPINE; CLOZAPINE-N-OXIDE; N-DESMETHYLCLOZAPINE; OLANZAPINE; RISPERIDONE; H-3 RECEPTORS; H-3 N-ALPHA-METHYLHISTAMINE BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
17
Recensione:
Indirizzi per estratti:
Citazione:
E. Schlicker e I. Marr, "THE MODERATE AFFINITY OF CLOZAPINE AT H-3 RECEPTORS IS NOT SHARED BY ITS 2 MAJOR METABOLITES AND BY STRUCTURALLY RELATED AND UNRELATED ATYPICAL NEUROLEPTICS", Naunyn-Schmiedeberg's archives of pharmacology, 353(3), 1996, pp. 290-294

Abstract

We determined the affinity and/or potency of Introduction two metabolites of clozapine (clozapine-N-oxide and N-desmethylclozapine) and of five atypical neuroleptics, chemically related (olanzapine) or unrelated to clozapine (remoxipride, risperidone, thioridazine, zotepine), atH-3 receptors. The specific binding of H-3-N-alpha-methylhistamine torat brain cortex homogenates was inhibited by the seven compounds; the pK(i) values were: N-desmethylclozapine (5.33); clozapine-N-oxide (4.18); olanzapine (5.45); thioridazine (4.91); zotepine (4.75); remoxipride (4.51) and risperidone (4.43). Three compounds were examined in afunctional H-3 receptor model as well. The electrically evoked tritium overflow from superfused mouse brain cortex slices, which representsquasiphysiological noradrenaline release, was not affected by N-desmethylclozapine (3.2 and 10 mu M), clozapine-N-oxide (3.2-100 mu M) and olanzapine (3.2-32 mu M). On the other hand, the three compounds shifted to the right the concentration-response curve of histamine for its inhibitory effect on the evoked overflow; the apparent pA(2) values were 5.84, 4.21 and 5.80, respectively. The present study shows that five atypical neuroleptics of different chemical classes and the two major metabolites of clozapine possess a lower affinity and/or antagonistic potency at H-3 receptors than clozapine itself (pK(i) 6.15, pA(2) 6.33; Kathmann M, Schlicker E,Gothert M (1994). Psychopharmacology 116: 464-468).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 10:32:38