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Antipsychotic drug action: antagonism, inverse agonism or partial agonism

Strange, P. G. (2008) Antipsychotic drug action: antagonism, inverse agonism or partial agonism. Trends in Pharmacological Sciences, 29 (6). pp. 314-321. ISSN 0165-6147

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To link to this article DOI: 10.1016/j.tips.2008.03.009

Abstract/Summary

The positive, psychotic symptoms of schizophrenia can be treated by antipsychotic drugs and it has been assumed that these are antagonists at the D-2 and D-3 dopamine receptors in the brain. Recently, the D-2/D-3 partial agonist aripiprazole has been introduced as an antipsychotic drug. It has also been realized that, using in vitro assays, the other antipsychotic drugs are in fact inverse agonists at D-2/D-3 dopamine receptors. This raises questions about how these disparate drugs can achieve a similar clinical outcome. In this review, I shall consider the efficacies of these drugs in signalling assays and how these efficacies might affect treatment outcomes. It seems that the treatment outcome might depend on the overall level of cell stimulation, which is in turn dependent on the level of residual dopamine and the efficacy of the drug in signalling assays.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
ID Code:13630
Uncontrolled Keywords:D-2 DOPAMINE-RECEPTOR, PROLACTIN-RELEASE, SCHIZOPHRENIA, ARIPIPRAZOLE, OCCUPANCY, MECHANISMS, HALOPERIDOL, ACTIVATION, EFFICACY, BINDING

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