ArticlePsychopharmacology2004
FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia.
Article in Psychopharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 37 citations in OpenAlex.
- Structural Basis for D3/D4-Selective Antagonism of Piperazinylalkyl Pyrazole/Isoxazole Analogs.Molecules (Basel, Switzerland) · 2025Article
- Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.eLife · 2019Article
- Buspirone Counteracts MK-801-Induced Schizophrenia-Like Phenotypes through Dopamine DFrontiers in pharmacology · 2017Article
- Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.Journal of medicinal chemistry · 2010Article
- Realistic expectations of prepulse inhibition in translational models for schizophrenia research.Psychopharmacology · 2008Review
- Disruption of prepulse inhibition of the startle reflex by the preferential D(3) agonist ropinirole in healthy males.Psychopharmacology · 2007Article
- Modulation of midbrain dopamine neurotransmission by serotonin, a versatile interaction between neurotransmitters and significance for antipsychotic drug action.Current neuropharmacology · 2006Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
rationale2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213) is a highly selective antagonist at the dopamine D(4) receptor subtype. It was designed as a derivative of two partial antagonists and has been proven to be a complete antagonist in mitogenesis assay.
objectivesIn the present study, FAUC 213 was examined for antipsychotic properties in animal models of behavioural neurobiology and neurochemistry.
methodsDifferent concentrations of FAUC 213 were screened for effects on spontaneous, as well as amphetamine-induced, locomotor activity and apomorphine-induced prepulse disruption. The liability of causing extrapyramidal side effects was investigated in models of catalepsy and by high-performance liquid chromatography (HPLC) detection of dopamine turnover in several brain regions. The application schedule was validated, and the bioavailability of the compound determined, by means of a HPLC-pharmacokinetic study.
resultsA significant effect in both the reduction of amphetamine-induced locomotor hyperactivity and the restoration of apomorphine-disrupted prepulse inhibition was found at 30 mg/kg. This dose proved not to be high enough to induce catalepsy or to increase dopamine turnover in the dorsal striatum, nucleus accumbens and medial prefrontal cortex. The selective D(4) antagonist FAUC 213, therefore, is not believed to mediate the above-mentioned effects via D(2) receptor antagonism, but a partial involvement of 5-HT(2)- and alpha(1)-receptors cannot be ruled out at present.
conclusionsWe have gathered evidence that FAUC 213 exhibits atypical antipsychotic characteristics.
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