Antipsychotic drug action: antagonism, inverse agonism or partial agonism.

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Strange PG

Antipsychotic drug action: antagonism, inverse agonism or partial agonism.

Trends Pharmacol Sci. 2008 Jun;29(6):314-21. doi: 10.1016/j.tips.2008.03.009. Epub 2008 May 28.

PubMed ID

18471899 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Promazine	Dopamine D2 receptor	Protein	Humans	Yes	Antagonist	Details
Propiomazine	Dopamine D2 receptor	Protein	Humans	Unknown	Antagonist	Details