SAR Study of 1-Aryl-4-(phenylarylmethyl)piperazines as Ligands for Both Dopamine D_2 and Serotonin 5-HT_<1A> Receptors Showing Varying Degrees of (Ant)agonism. Selection of a Potential Atypical Antipsychotic

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The syntheses of several 1-aryl-4-(arylpyridylmethyl)piperazines (4) and their affinities for dopamine D_2 and serotonin 5-HT_<1A> receptors are described. The compounds were evaluated both in vitro and in vivo, resulting in the identification of the drug candidate SLV313 (4e) with equipotent and full D_2 receptor antagonism and 5-HT_<1A> receptor agonism. Minor structural modifications in SLV313 revealed the possibility of designing compounds possessing varying degrees of partial agonism on one or both target receptors.
公益社団法人日本薬学会の論文
2006-09-01