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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. Copyright © 2012 Elsevier Ltd. All rights reserved.


Floriane Mangin, Sébastien Dilly, Benoît Joly, Jacqueline Scuvée-Moreau, Jon Evans, Vincent Setola, Bryan L Roth, Jean-François Liégeois. Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. Bioorganic & medicinal chemistry letters. 2012 Jul 15;22(14):4550-4

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PMID: 22738628

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