Abstract
We examined possible interactions between neuroleptics and the histamine H3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H3 antagonist, [125I]-iodophenpropit, we observed a Ki of 236 +/- 87 nM. Functionally, clozapine was studied on the H3-mediated inhibition of [3H]-5-hydroxytryptamine ([3H]-5-HT) release from rat brain cortex slices. Clozapine acts as an antagonist with an apparent KB value of 79.5 nM.
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- Baldessarini R. J., Centorrino F., Flood J. G., Volpicelli S. A., Huston-Lyons D., Cohen B. M. Tissue concentrations of clozapine and its metabolites in the rat. Neuropsychopharmacology. 1993 Sep;9(2):117–124. doi: 10.1038/npp.1993.50. [DOI] [PubMed] [Google Scholar]
- Baldessarini R. J., Frankenburg F. R. Clozapine. A novel antipsychotic agent. N Engl J Med. 1991 Mar 14;324(11):746–754. doi: 10.1056/NEJM199103143241107. [DOI] [PubMed] [Google Scholar]
- Deutsch S. I., Rosse R. B., Kendrick K. A., Fay-McCarthy M., Collins J. P., Jr, Wyatt R. J. Famotidine adjunctive pharmacotherapy for schizophrenia: preliminary data. Clin Neuropharmacol. 1993 Dec;16(6):518–524. [PubMed] [Google Scholar]
- Fink K., Schlicker E., Neise A., Göthert M. Involvement of presynaptic H3 receptors in the inhibitory effect of histamine on serotonin release in the rat brain cortex. Naunyn Schmiedebergs Arch Pharmacol. 1990 Nov;342(5):513–519. doi: 10.1007/BF00169038. [DOI] [PubMed] [Google Scholar]
- Jansen F. P., Wu T. S., Voss H. P., Steinbusch H. W., Vollinga R. C., Rademaker B., Bast A., Timmerman H. Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br J Pharmacol. 1994 Oct;113(2):355–362. doi: 10.1111/j.1476-5381.1994.tb16995.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kaminsky R., Moriarty T. M., Bodine J., Wolf D. E., Davidson M. Effect of famotidine on deficit symptoms of schizophrenia. Lancet. 1990 Jun 2;335(8701):1351–1352. doi: 10.1016/0140-6736(90)91237-5. [DOI] [PubMed] [Google Scholar]
- Nakai T., Kitamura N., Hashimoto T., Kajimoto Y., Nishino N., Mita T., Tanaka C. Decreased histamine H1 receptors in the frontal cortex of brains from patients with chronic schizophrenia. Biol Psychiatry. 1991 Aug 15;30(4):349–356. doi: 10.1016/0006-3223(91)90290-3. [DOI] [PubMed] [Google Scholar]
- Prell G. D., Green J. P., Kaufmann C. A., Khandelwal J. K., Morrishow A. M., Kirch D. G., Linnoila M., Wyatt R. J. Histamine metabolites in cerebrospinal fluid of patients with chronic schizophrenia: their relationships to levels of other aminergic transmitters and ratings of symptoms. Schizophr Res. 1995 Jan;14(2):93–104. doi: 10.1016/0920-9964(94)00034-6. [DOI] [PubMed] [Google Scholar]
- Van der Werf J. F., Bast A., Bijloo G. J., Van der Vliet A., Timmerman H. HA autoreceptor assay with superfused slices of rat brain cortex and electrical stimulation. Eur J Pharmacol. 1987 Jun 19;138(2):199–206. doi: 10.1016/0014-2999(87)90433-x. [DOI] [PubMed] [Google Scholar]