SAR Study of 1-Aryl-4-(phenylarylmethyl)piperazines as Ligands for Both Dopamine D2 and Serotonin 5-HT1A Receptors Showing Varying Degrees of (Ant)agonism. Selection of a Potential Atypical Antipsychotic

Roelof Willem Feenstra; Adri van den Hoogenband; Cornelis Nicolaas Jozef Stroomer; Herman Heinrich van Stuivenberg; Martin Theodorus Maria Tulp; Stephen Kenneth Long; Johannes Antonius Maria van der Heyden; Cornelis Gerrit Kruse

doi:10.1248/cpb.54.1326

Notes

SAR Study of 1-Aryl-4-(phenylarylmethyl)piperazines as Ligands for Both Dopamine D₂ and Serotonin 5-HT_1A Receptors Showing Varying Degrees of (Ant)agonism. Selection of a Potential Atypical Antipsychotic

Roelof Willem Feenstra, Adri van den Hoogenband, Cornelis Nicolaas Jozef Stroomer, Herman Heinrich van Stuivenberg, Martin Theodorus Maria Tulp, Stephen Kenneth Long, Johannes Antonius Maria van der Heyden, Cornelis Gerrit Kruse

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Keywords: SLV313, N-phenylpiperazines, biaryl, (partial) dopamine D₂ receptor antagonist, (partial) serotonin 5-HT_1A receptor agonist, atypical antipsychotic

JOURNAL FREE ACCESS

2006 Volume 54 Issue 9 Pages 1326-1330

DOI https://doi.org/10.1248/cpb.54.1326

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Abstract

The syntheses of several 1-aryl-4-(arylpyridylmethyl)piperazines (4) and their affinities for dopamine D₂ 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 D₂ 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.

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