D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs |
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| Authors: | B. L. Roth S. Tandra L. H. Burgess D. R. Sibley H. Y. Meltzer |
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| Affiliation: | (1) Department of Psychiatry, Case Western Reserve University School of Medicine, Wood Building, W428, 44106-4935 Cleveland, OH, USA;(2) Department of Biochemistry, Case Western Reserve University School of Medicine, Wood Building, W428, 44106-4935 Cleveland, OH, USA;(3) Molecular Neuropharmacology Section, Experimental Therapeutics Branch, NINDS-NIH, National Institutes of Health, 20892 Bethesda, MD, USA |
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| Abstract: | The affinities of 13 atypical and 12 typical antipsychotic drugs for the cloned rat D4 dopamine receptor and the D4/D2 ratios were examined. Of the atypical antipsychotic drugs tested, only clozapine, risperidone, olanzapine, zotepine and tiospirone had affinities less than 20 nM. In fact, many atypical antipsychotic drugs had relatively low affinities for the cloned rat D4 receptor, with Ki values greater than 100 nM (Seroquel, fluperlapine, tenilapine, FG5803 and melperone). Additionally, several typical antipsychotic drugs had high affinities for the cloned rat D4 receptor, with Kis less than 20 nM (loxapine, chlorpromazine, fluphenazine, mesoridazine, thioridazine and trifluoroperazine). The ratios of D2/D4 affinities did not differentiate between these two types of antipsychotic drugs. Thus, D4 dopamine receptor affinity, used as a single measure, does not distinguish between the group of typical and atypical antipsychotic drugs analyzed. |
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| Keywords: | Antipsychotic drugs D4 dopamine receptor Rat |
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