Discovery of 1-[2-(2, 4-dimethylphenylsulfanyl) phenyl] piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder

B Bang-Andersen, T Ruhland…

Index: Bang-Andersen, Benny; Ruhland, Thomas; Jorgensen, Morten; Smith, Garrick; Frederiksen, Kristen; Jensen, Klaus Gjervig; Zhong, Huailing; Nielsen, Soren Moller; Hogg, Sandra; Mork, Arne; Stensbol, Tine Bryan Journal of Medicinal Chemistry, 2011 , vol. 54, # 9 p. 3206 - 3221

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Citation Number: 199

Abstract

The synthesis and structure− activity relationship of a novel series of compounds with combined effects on 5-HT3A and 5-HT1A receptors and on the serotonin (5-HT) transporter (SERT) are described. Compound 5m (Lu AA21004) was the lead compound, displaying high affinity for recombinant human 5-HT1A (K i= 15 nM), 5-HT1B (K i= 33 nM), 5-HT3A (K i= 3.7 nM), 5-HT7 (K i= 19 nM), and noradrenergic β1 (K i= 46 nM) receptors, and SERT (K i= ...