Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-D-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder

(R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169) and the phosphate prodrug 4-((3S,4S)-3-fluoro-1-((R)-1-(4-methylbenzyl)-2-oxopyrrolidin-3-yl)piperidin-4-yl)phenyl dihydrogen phosphate (BMS-986163) were identified from a drug discovery effort...

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Veröffentlicht in:	The Journal of pharmacology and experimental therapeutics 2017-12, Vol.363 (3), p.377-393
Hauptverfasser:	Bristow, Linda J., Gulia, Jyoti, Weed, Michael R., Srikumar, Bettadapura N., Li, Yu-Wen, Graef, John D., Naidu, Pattipati S., Sanmathi, Charulatha, Aher, Jayant, Bastia, Tanmaya, Paschapur, Mahesh, Kalidindi, Narasimharaju, Kumar, Kuchibhotla Vijaya, Molski, Thaddeus, Pieschl, Rick, Fernandes, Alda, Brown, Jeffrey M., Sivarao, Digavalli V., Newberry, Kimberly, Bookbinder, Mark, Polino, Joseph, Keavy, Deborah, Newton, Amy, Shields, Eric, Simmermacher, Jean, Kempson, James, Li, Jianqing, Zhang, Huiping, Mathur, Arvind, Kallem, Raja Reddy, Sinha, Meenakshee, Ramarao, Manjunath, Vikramadithyan, Reeba K., Thangathirupathy, Srinivasan, Warrier, Jayakumar, Islam, Imadul, Bronson, Joanne J., Olson, Richard E., Macor, John E., Albright, Charlie F., King, Dalton, Thompson, Lorin A., Marcin, Lawrence R., Sinz, Michael
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Intravenous Allosteric Regulation Animals Antidepressive Agents - adverse effects Antidepressive Agents - pharmacokinetics Antidepressive Agents - therapeutic use Brain - drug effects Brain - metabolism Brain - physiopathology Brain Waves - drug effects Depressive Disorder, Major - drug therapy Depressive Disorder, Major - physiopathology Depressive Disorder, Major - psychology Dissociative Disorders - chemically induced Macaca fascicularis Male Memory, Short-Term - drug effects Mice Motor Activity - drug effects Organophosphates - adverse effects Organophosphates - pharmacokinetics Organophosphates - therapeutic use Piperidines - adverse effects Piperidines - pharmacokinetics Piperidines - therapeutic use Prodrugs - adverse effects Prodrugs - pharmacokinetics Prodrugs - therapeutic use Pyrrolidinones - adverse effects Pyrrolidinones - pharmacokinetics Pyrrolidinones - therapeutic use Radioligand Assay Rats, Sprague-Dawley Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - metabolism Xenopus
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