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  • Title: Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
    Author: Leslie CP, Biagetti M, Bison S, Bromidge SM, Di Fabio R, Donati D, Falchi A, Garnier MJ, Jaxa-Chamiec A, Manchee G, Merlo G, Pizzi DA, Stasi LP, Tibasco J, Vong A, Ward SE, Zonzini L.
    Journal: J Med Chem; 2010 Dec 09; 53(23):8228-40. PubMed ID: 21053897.
    Abstract:
    In an effort to identify selective drug like pan-antagonists of the 5-HT1 autoreceptors, studies were conducted to elaborate a previously reported dual acting 5-HT1 antagonist/SSRI structure. A novel series of compounds was identified showing low intrinsic activities and potent affinities across the 5-HT1A, 5-HT1B, and 5-HT1D receptors as well as high selectivity against the serotonin transporter. From among these compounds, 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (36) was found to combine potent in vivo activity with a strong preclinical developability profile, and on this basis it was selected as a drug candidate with the aim of assessing its potential as a fast-onset antidepressant/anxiolytic.
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