Evidence that clozapine directly interacts on the GABAB receptor.
| Autor: | Wu Y; Program in Neuroscience and Mental Health, University of Toronto fCentre for Addiction and Mental Health, Toronto, Ontario, Canada., Blichowski M, Daskalakis ZJ, Wu Z, Liu CC, Cortez MA, Snead OC 3rd |
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| Jazyk: | angličtina |
| Zdroj: | Neuroreport [Neuroreport] 2011 Sep 14; Vol. 22 (13), pp. 637-41. |
| DOI: | 10.1097/WNR.0b013e328349739b |
| Abstrakt: | Neurophysiological studies suggest that clozapine may facilitate γ-aminobutyric acid (GABAergic) neurotransmission. Therefore, we studied the interaction between clozapine and the GABAB receptor (GABABR). We showed that clozapine, and not N-desmethylclozapine, which is a metabolite of clozapine, increased the binding of the GABABR antagonist, [³H]-CGP54626A, at GABABRs. Linear regression analysis showed that the correlation between the dose of clozapine and the increase of [³H]-CGP54626A binding was significant. The curve of specific [³H]-CGP54626A binding in competition with different concentrations of GABA was left shifted in the presence of clozapine. With HEK293 cells overexpressing GABABR, we showed that clozapine had a significant increase of [³H]-CGP54626A binding at GABABR1 subunit, which provided a clue of the potential therapeutic target of clozapine. (2011 Wolters Kluwer Health | Lippincott Williams & Wilkins.) |
| Databáze: | MEDLINE |
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