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Chemical Compound Review:

Bifeprunox 7-[4-[(3- phenylphenyl)methyl]piperazin- 1...

Synonyms: Bifeprunoxum, CHEMBL218166, SureCN114371, AG-F-20686, CHEBI:467160, ...

Cosi, C. et al., Assié, M.B. et al., Bardin, L. et al., Kleven, M.S. et al.

Bardin, Kleven, Barret-Grévoz, Depoortère, Newman-Tancredi,

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Disease relevance of DU127090

When 5-HT1A receptors were blocked by pretreatment with WAY100635 (2.5 mg/kg, s.c.), cataleptogenic properties of SSR181507 and sarizotan were unmasked, and the catalepsy induced by bifeprunox was enhanced [1].

High impact information on DU127090

In contrast, SSR181507 and bifeprunox potently inhibited both CLP and bar catalepsy [2].
Hippocampal 5-HT was decreased by bifeprunox, SSR181507, SLV313, sarizotan, and nemonapride, effects similar to those seen with the 5-HT1A agonist, (+)-8-hydroxy-2-(di-n-propylamino)tetralin [(+)8-OH-DPAT], consistent with activation of 5-HT1A autoreceptors [3].
Bifeprunox only weakly increased prolactin at high doses (13 ng/ml at 40 mg/kg) and clozapine only affected prolactin at the highest dose tested (41 ng/ml at 40 mg/kg) [4].

Associations of DU127090 with other chemical compounds

Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release [4].

References

Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties. Bardin, L., Kleven, M.S., Barret-Grévoz, C., Depoortère, R., Newman-Tancredi, A. Neuropsychopharmacology (2006) [Pubmed]
Novel antipsychotic agents with 5-HT(1A) agonist properties: role of 5-HT(1A) receptor activation in attenuation of catalepsy induction in rats. Kleven, M.S., Barret-Grévoz, C., Slot, L.B., Newman-Tancredi, A. Neuropharmacology (2005) [Pubmed]
Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain. Assié, M.B., Ravailhe, V., Faucillon, V., Newman-Tancredi, A. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Cosi, C., Carilla-Durand, E., Assié, M.B., Ormiere, A.M., Maraval, M., Leduc, N., Newman-Tancredi, A. Eur. J. Pharmacol. (2006) [Pubmed]

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