Trifluoperazine, an orally available clinically used drug, disrupts opioid antinociceptive tolerance
by
Tang L, Shukla PK, Wang ZJ.
Department of Biopharmaceutical Sciences,
College of Pharmacy,
University of Illinois,
833 South Woods Street,
Chicago, IL 60612, USA.
Neurosci Lett. 2006 Apr 10-17;397(1-2):1-4.

ABSTRACT

Calcium/calmodulin dependent protein kinase II (CaMKII) has been shown to play an important role in the generation and maintenance of opioid tolerance. In this study, trifluoperazine was studied for its effect on morphine tolerance in mice. Acute treatment with trifluoperazine (0.5 mg/kg, i.p.) completely reversed the established antinociceptive tolerance to morphine. Pretreatment with trifluoperazine also significantly attenuated the development of antinociceptive tolerance (p<0.01). Morphine induced a significant up-regulation of supraspinal and spinal CaMKII activity in tolerant mice, which was abolished after the pretreatment or acute treatment with trifluoperazine. These data suggested that trifluoperazine was capable of suppressing opioid tolerance, possibly by the mechanism of inhibiting CaMKII. Since trifluoperazine has been safely used as an antipsychotic drug, we propose that the drug should be studied in humans for the prevention and treatment of opioid tolerance and addiction.

Pain
CREB
DAMGO
G protein
Morphine
Tramadol
Methadone
Oxycodone
Endomorphins
Glycine anatagonists
Fentanyl and ketamine
The extended amygdala
NSAIDs/opioid tolerance
Opioid receptor migration
Opioids, mood and cognition
Morphine, naltrexone and tolerance
Anxiety, opioids, cholecystokinin and tolerance

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