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  • Title: Novel, flexible, and conformationally defined analogs of gepirone: synthesis and 5-HT1A, 5-HT2A, and D2 receptor activity.
    Author: Paluchowska MH, Bugno R, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Tatarczyńska E, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E.
    Journal: Bioorg Med Chem; 2005 Feb 15; 13(4):1195-200. PubMed ID: 15670928.
    Abstract:
    Novel, flexible arylpiperazine gepirone analogs (1a-3a) with a mixed 5-HT1A/5-HT2A receptor profile, low D2 receptor affinity, and agonistic (2a) or partial agonistic (1a, 3a) activity toward 5-HT1A receptor sites were synthesized. Their conformationally restricted counterparts (1b-3b) were selective 5-HT1A ligands (over 5-HT2A and D2 receptors), which turned out to be agonists (2b, 3b), or partial agonist (1b) of 5-HT1A receptors.
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