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  • Title: Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.
    Author: Mangin F, Dilly S, Joly B, Scuvée-Moreau J, Evans J, Setola V, Roth BL, Liégeois JF.
    Journal: Bioorg Med Chem Lett; 2012 Jul 15; 22(14):4550-4. PubMed ID: 22738628.
    Abstract:
    The selectivity for 5-HT(1A) versus D(4) receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tetrahydropyridine compounds (3i-l) have a higher affinity for 5-HT(1A) receptors than do the corresponding unsubstituted phenylpiperazine analogues (3e-h). Compounds 3e and 3i appear to be selective for 5-HT(1A) receptors over other relevant receptors and still behave as neutral antagonists.
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