| 16946546 |
Feenstra RW, van den Hoogenband A, Stroomer CN, van Stuivenberg HH, Tulp MT, Long SK, van der Heyden JA, Kruse CG: 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. Chem Pharm Bull. 2006 Sep;54(9):1326-30.
Selection of a potential atypical antipsychotic.. 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. |
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