Journal
LIFE SCIENCES
Volume 68, Issue 1, Pages 29-39Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0024-3205(00)00911-5
Keywords
histamine H-1 receptor; muscarinic receptor; alpha(1)-adrenoceptor; alpha(2)-adrenoceptor; dopamine D-2 receptor; serotonin 5-HT1A receptor; serotonin 5-HT2A receptor
Funding
- NIMH NIH HHS [MH/NS 31862] Funding Source: Medline
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Using radioligand binding assays and post-mortem normal human brain tissue, we obtained equilibrium dissociation constants (K(d)s) for nine new antipsychotic drugs (iloperidone, melperone, olanzapine, ORG 5222, quetiapine, risperidone, sertindole, ziprasidone, and zotepine), one metabolite of a new drug (9-OH-risperidone), and three older antipsychotics (clozapine, haloperidol, and pimozide) at nine different receptors (alpha (1)-adrenergic, alpha (2)-adrenergic, dopamine D-2, histamine H-1, muscarinic, and serotonin 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors). Iloperidone was the most potent drug at the two adrenergic receptors. ORG 5222 was the most potent drug at dopamine D-2 and 5-HT2c receptors, while ziprasidone was the most potent compound at three serotonergic receptors (5-HT1A, 5-HT1D, and 5-HT2A). At the remaining two receptors, olanzapine was the most potent drug at the histamine H-1 receptor (K-d=0.087 nM); clozapine at the muscarinic receptor (K-d=9 nM). Certain therapeutic and adverse effects, as well as certain drug interactions can be predicted from a drug's potency for blocking a specific receptor. These data can provide guidelines for the clinician in the choice of antipsychotic drug. (C) 2000 Elsevier Science Inc. All rights reserved.
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