New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.

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Feenstra RW, de Moes J, Hofma JJ, Kling H, Kuipers W, Long SK, Tulp MT, van der Heyden JA, Kruse CG

New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2345-9.

PubMed ID

11527728 [ View in PubMed

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Abstract

This paper describes the syntheses of several 1-aryl-4-(biarylmethylene)piperazines and the results of the determination of their affinity for D(2) and 5-HT(1A) receptors. A selection of these compounds was evaluated in vivo, resulting in the identification of a drug candidate which is being clinically evaluated as a potential atypical antipsychotic with reduced extrapyrimidal side effects.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bifeprunox	5-hydroxytryptamine receptor 1A	Ki (nM)	9.3	N/A	N/A	Details
Bifeprunox	Dopamine D2 receptor	Ki (nM)	2.2	N/A	N/A	Details
Clozapine	5-hydroxytryptamine receptor 1A	Ki (nM)	270	N/A	N/A	Details
Clozapine	Dopamine D2 receptor	Ki (nM)	69	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	1.4	N/A	N/A	Details