Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors |
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| Authors: | Mangin Floriane Dilly Sébastien Joly Benoît Scuvée-Moreau Jacqueline Evans Jon Setola Vincent Roth Bryan L Liégeois Jean-François |
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| Institution: | 1. Laboratory of Medicinal Chemistry and Drug Research Center, University of Liège, Avenue de l’Hôpital, 1 (B36), B-4000 Liège 1, Belgium;2. Laboratory of Pharmacology and GIGA-Neuroscience, University of Liège, Avenue de l’Hôpital, 1 (B36), B-4000 Liège 1, Belgium;3. Department of Pharmacology School of Medicine and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, 4072 Genetic Medicine Building, CB# 7365, Chapel Hill, NC 27599, USA;4. National Institute of Mental Health Psychoactive Drug Screening Program, Department of Pharmacology, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC 27599, USA |
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| 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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