Behavioral and neurochemical effects of the preferential dopamine D3 receptor agonist cis-8-OH-PBZI

European Journal of Pharmacology
A Fink-JensenM A Scheideler

Abstract

In the present study we investigated the in vivo pharmacological profile of the benz[e]indole cis-8-hydroxy-3-(n-propyl)],2,3a,4,5,9b-hexahydro-1H-benz[e]indole (cis-8-OH-PBZI), which has been described as a preferential dopamine D3 receptor agonist in vitro. The compound inhibited spontaneous locomotor activity in mice, an effect which was antagonized by the dopamine D3 receptor antagonist 5,6-dimethoxy-2-(di-u-propylamino) indan (U99194A). Moreover, cis-8-OH-PBZI inhibited conditioned avoidance responding in rats, a preclinical test indicative of antipsychotic efficacy, at doses which did not induce catalepsy. Doses of cis-8-OH-PBZI (6 and 12 mg/kg) that inhibited spontaneous locomotor activity in rats did not affect interstitial levels of dopamine and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens or dorsolateral striatum. In contrast to the effect of the dopamine receptor agonist (+/-)-2-dipropylamino-7-hydroxy-1,2,3,4-tetrahydronaphythalene (7-OH-DPAT), cis-8-OH-PBZI did not induce locomotor activity in reserpinized mice. In conclusion, cis-8-OH-PBZI exhibits a pharmacological profile that suggests it has antipsychotic activity but lacks the motoric side effects often associated with antipsychotic medication. ...Continue Reading

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Citations

May 2, 2012·Pharmaceutical Research·E V Kuzhikandathil, S Kortagere
Jun 23, 2001·Pharmacology, Biochemistry, and Behavior·H FrancesJ Bourre
Nov 5, 2002·Journal of Ethnopharmacology·Monrudee SukmaHiroshi Watanabe
Sep 11, 2008·Pharmacogenomics·Bk ThelmaArun Kumar Tiwari
Aug 11, 2004·Pharmacology, Biochemistry, and Behavior·Peter MalikLinda Peacock
Feb 17, 2009·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Clement C ZaiJames L Kennedy

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