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Dopamine D2(High) receptors moderately elevated by sertindole.

Philip Seeman¹

¹Department of Pharmacology, Medical Science Building, University of Toronto, Toronto, Ontario, Canada M5S 1A8. philip.seeman@utoronto.ca

Synapse (New York, N.Y.)

|February 23, 2008

Summary

The antipsychotic sertindole increased dopamine D2(High) receptors in rats, suggesting potential dopamine supersensitivity. This biochemical change was less pronounced than with haloperidol.

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Area of Science:

Neuropharmacology
Psychiatry

Background:

Long-term antipsychotic use can lead to behavioral dopamine supersensitivity.
This phenomenon is linked to increased dopamine D2 receptor high-affinity states (D2(High)) in rat striata.

Purpose of the Study:

To investigate if the antipsychotic sertindole induces biochemical changes associated with dopamine supersensitivity.
To quantify the effect of sertindole on dopamine D2(High) receptors.

Main Methods:

Rats were administered sertindole subcutaneously at 1.25 mg/kg/day for nine days.
The proportion of D2(High) receptors in homogenized striata was measured.

Main Results:

Sertindole administration significantly increased the proportion of D2(High) receptors by 186%–215%.
The total D2 receptor population remained unchanged.
The observed increase in D2(High) receptors was less than that reported for haloperidol.

Conclusions:

Sertindole treatment in rats elicits biochemical changes indicative of dopamine supersensitivity.
These findings suggest that sertindole may induce behavioral dopamine supersensitivity in rats and potentially in patients.
The magnitude of this effect is lower compared to haloperidol.