The Synthesis and Biological Evaluation of Quinolyl-piperazinyl Piperidines as Potent Serotonin 5-HT1AAntagonists

Autor: Shen Z, Tom A. Comery, David Smith, Brian J. Platt, Terrance H. Andree, Zhang Minsheng, Magid Abou-Gharbia, Sukoff-Rizzo Sj, Havran Lm, Chong Dc, Natasha Kagan, Zoë A. Hughes, Kelly Sullivan, Bach Ac rd, Boyd L. Harrison, Wayne E. Childers, Magda Asselin, Sharon Rosenzweig-Lipson, Claudine Pulicicchio, Steven M. Grauer, Marathias, George Theodore Grosu, Mark Day, Bicksler Jj, Chad E. Beyer, Adedayo Adedoyin, Christine Huselton, Sabb Al, Suzan Aschmies, Ronald L. Magolda, Warren D. Hirst, Kleintop T, Albert J. Robichaud

Publikováno v: Journal of Medicinal Chemistry. 53:4066-4084

As part of an effort to identify 5-HT(1A) antagonists that did not possess typical arylalkylamine or keto/amido-alkyl aryl piperazine scaffolds, prototype compound 10a was identified from earlier work in a combined 5-HT(1A) antagonist/SSRI program. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8128f3b71923ae4c75a96a7c24e6d62e
https://doi.org/10.1021/jm1000908

A framework for translating tauopathy therapeutics: Drug discovery to clinical trials.

Autor: Feldman HH; Department of Neurosciences, University of California San Diego, La Jolla, California, USA., Cummings JL; Chambers-Grundy Center for Transformative Neuroscience, Department of Brain Health, School of Integrated Health Sciences, University of Nevada at Las Vegas, Las Vegas, Nevada, USA., Boxer AL; Department of Neurology, Memory and Aging Center, University of California San Francisco, San Francisco, California, USA., Staffaroni AM; Department of Neurology, Memory and Aging Center, University of California San Francisco, San Francisco, California, USA., Knopman DS; Department of Neurology, Mayo Clinic, Rochester, Minnesota, USA., Sukoff Rizzo SJ; Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Territo PR; Department of Medicine, Division of Clinical Pharmacology, Indiana University School of Medicine, Indianapolis, Indiana, USA., Arnold SE; Department of Neurology, Harvard Medical School, Massachusetts General Hospital, Charlestown, Massachusetts, USA., Ballard C; College of Medicine and Health, University of Exeter, Exeter, UK., Beher D; Asceneuron, Lausanne, Switzerland., Boeve BF; Department of Neurology, Mayo Clinic, Rochester, Minnesota, USA., Dacks PA; The Association for Frontotemporal Degeneration, King of Prussia, Pennsylvania, USA., Diaz K; CurePSP, New York, New York, USA., Ewen C; UCB Pharma, Slough, UK., Fiske B; The Michael J. Fox Foundation for Parkinson's Research, New York, New York, USA., Gonzalez MI; Drug Discovery and Development Consultants, Cambridge, UK., Harris GA; Rainwater Charitable Foundation, Fort Worth, Texas, USA., Hoffman BJ; Origami Therapeutics, San Diego, California, USA., Martinez TN; Critical Path Institute, Tucson, Arizona, USA., McDade E; Department of Neurology, Washington University School of Medicine, St. Louis, Missouri, USA., Nisenbaum LK; Alzheimer's Drug Discovery Foundation, New York, New York, USA., Palma JA; Novartis Institutes for Biomedical Research, Cambridge, Massachusetts, USA.; Department of Neurology, New York University Grossman School of Medicine, New York, New York, USA., Quintana M; Berry Consultants, Austin, Texas, USA., Rabinovici GD; Department of Neurology, Memory and Aging Center, University of California San Francisco, San Francisco, California, USA., Rohrer JD; Department of Neurodegenerative Disease, Dementia Research Centre, Queen Square Institute of Neurology, University College of London, London, UK., Rosen HJ; Department of Neurology, Memory and Aging Center, University of California San Francisco, San Francisco, California, USA., Troyer MD; Denali Therapeutics, South San Francisco, California, USA., Kim DY; Department of Neurology, Genetics and Aging Research Unit, McCance Center for Brain Health, Mass General Institute for Neurodegenerative Disease, Massachusetts General Hospital, Charlestown, Massachusetts, USA., Tanzi RE; Department of Neurology, Genetics and Aging Research Unit, McCance Center for Brain Health, Mass General Institute for Neurodegenerative Disease, Massachusetts General Hospital, Charlestown, Massachusetts, USA., Zetterberg H; Department of Psychiatry and Neurochemistry, Sahlgrenska Academy at the University of Gothenburg, Mölndal, Sweden., Ziogas NK; Biogen, Cambridge, Massachusetts, USA., May PC; ADvantage Neuroscience Consulting LLC, Fort Wayne, Indiana, USA., Rommel A; Rainwater Charitable Foundation, Fort Worth, Texas, USA.

Publikováno v: Alzheimer's & dementia : the journal of the Alzheimer's Association [Alzheimers Dement] 2024 Nov; Vol. 20 (11), pp. 8129-8152. Date of Electronic Publication: 2024 Sep 24.

Characterizing molecular and synaptic signatures in mouse models of late-onset Alzheimer's disease independent of amyloid and tau pathology.

Autor: Kotredes KP; The Jackson Laboratory, Bar Harbor, Maine, USA., Pandey RS; The Jackson Laboratory for Genomic Medicine, Farmington, Connecticut, USA., Persohn S; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Elderidge K; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Burton CP; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Miner EW; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Haynes KA; Department of Medicine, University of Pittsburgh Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Santos DFS; Department of Medicine, University of Pittsburgh Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Williams SP; Department of Medicine, University of Pittsburgh Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Heaton N; Department of Medicine, University of Pittsburgh Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Ingraham CM; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Lloyd C; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA., Garceau D; The Jackson Laboratory, Bar Harbor, Maine, USA., O'Rourke R; The Jackson Laboratory, Bar Harbor, Maine, USA., Herrick S; The Jackson Laboratory, Bar Harbor, Maine, USA., Rangel-Barajas C; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis, Indiana, USA., Maharjan S; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA.; Department of Radiology & Imaging Sciences, Indiana University School of Medicine, Indianapolis, Indiana, USA., Wang N; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA.; Department of Radiology & Imaging Sciences, Indiana University School of Medicine, Indianapolis, Indiana, USA., Sasner M; The Jackson Laboratory, Bar Harbor, Maine, USA., Lamb BT; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA.; Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis, Indiana, USA., Territo PR; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA.; Department of Medicine, Division of Clinical Pharmacology, Indiana University School of Medicine, Indianapolis, Indiana, USA., Sukoff Rizzo SJ; Department of Medicine, University of Pittsburgh Aging Institute, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA., Carter GW; The Jackson Laboratory, Bar Harbor, Maine, USA.; The Jackson Laboratory for Genomic Medicine, Farmington, Connecticut, USA.; Tufts University Graduate School of Biomedical Sciences, Boston, Massachusetts, USA.; Graduate School of Biomedical Sciences and Engineering, University of Maine, Orono, Maine, USA., Howell GR; The Jackson Laboratory, Bar Harbor, Maine, USA.; Tufts University Graduate School of Biomedical Sciences, Boston, Massachusetts, USA.; Graduate School of Biomedical Sciences and Engineering, University of Maine, Orono, Maine, USA., Oblak AL; Indiana University School of Medicine, Indianapolis, Indiana, USA.; Stark Neurosciences Research Institute, Indianapolis, Indiana, USA.; Department of Radiology & Imaging Sciences, Indiana University School of Medicine, Indianapolis, Indiana, USA.

Publikováno v: Alzheimer's & dementia : the journal of the Alzheimer's Association [Alzheimers Dement] 2024 Jun; Vol. 20 (6), pp. 4126-4146. Date of Electronic Publication: 2024 May 12.

Validation and in vivo characterization of research antibodies for Moesin, CD44, Midkine, and sFRP-1.

Autor: Doolen S; Aging Institute, University of Pittsburgh, Pittsburgh, Pennsylvania, 15219, USA., Ayoubi R; Neurology and Neurosurgery, McGill University, Montreal, Québec, H3A 2B4, Canada., Laflamme C; Neurology and Neurosurgery, McGill University, Montreal, Québec, H3A 2B4, Canada., Betarbet R; Center for Neurodegenerative Disease, Emory University, Atlanta, Georgia, 30322, USA.; Department of Pharmacology, Emory University, Atlanta, Georgia, 30322, USA., Zoeller E; Department of Pharmacology, Emory University, Atlanta, Georgia, 30322, USA., Williams SG; Aging Institute, University of Pittsburgh, Pittsburgh, Pennsylvania, 15219, USA., Fu H; Department of Pharmacology, Emory University, Atlanta, Georgia, 30322, USA.; Chemical Biology Discovery Center, Emory University, Atlanta, Georgia, 30322, USA.; Winship Cancer Institute, Emory University, Atlanta, Georgia, 30322, USA., Levey AI; Neurology, Emory University, Atlanta, Georgia, 30322, USA.; Goizueta Alzheimer's Disease Research Center, Emory University, Atlanta, Georgia, USA., Sukoff Rizzo SJ; Aging Institute, University of Pittsburgh, Pittsburgh, Pennsylvania, 15219, USA.

Publikováno v: F1000Research [F1000Res] 2024 Apr 23; Vol. 12, pp. 1070. Date of Electronic Publication: 2024 Apr 23 (Print Publication: 2023).

Discovery and validation of genes driving drug-intake and related behavioral traits in mice.

Autor: Roy TA; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Bubier JA; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Dickson PE; Joan C Edwards School of Medicine, Marshall University, Huntington, West Virginia, USA., Wilcox TD; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Ndukum J; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Clark JW; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Sukoff Rizzo SJ; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA.; School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania, USA., Crabbe JC; VA Portland Health Care System, Oregon Health & Science University, Portland, Oregon, USA., Denegre JM; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Svenson KL; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Braun RE; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Kumar V; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Murray SA; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., White JK; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Philip VM; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA., Chesler EJ; Center for Addiction Biology, The Jackson Laboratory, Bar Harbor, Maine, USA.

Publikováno v: Genes, brain, and behavior [Genes Brain Behav] 2024 Jan 02, pp. e12875. Date of Electronic Publication: 2024 Jan 02.