Preclinical validation of [18F]2FNQ1P as a specific PET radiotracer of 5-HT6 receptors in rat, pig, non-human primate and human brain tissue.

[1]  R. Nirogi,et al.  SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization , 2019, Behavioural pharmacology.

[2]  R. Khoury,et al.  The role of 5 HT6-receptor antagonists in Alzheimer’s disease: an update , 2018, Expert opinion on investigational drugs.

[3]  T. Fullerton,et al.  A Phase 2 clinical trial of PF-05212377 (SAM-760) in subjects with mild to moderate Alzheimer’s disease with existing neuropsychiatric symptoms on a stable daily dose of donepezil , 2018, Alzheimer's Research & Therapy.

[4]  A. Bojarski,et al.  Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties. , 2018, European journal of medicinal chemistry.

[5]  D. Bennett.  Lack of Benefit With Idalopirdine for Alzheimer Disease: Another Therapeutic Failure in a Complex Disease Process. , 2018, JAMA.

[6]  M. Kołaczkowski,et al.  Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating , 2018, Metabolic Brain Disease.

[7]  L. Tremblay,et al.  Characterization and Reliability of [18F]2FNQ1P in Cynomolgus Monkeys as a PET Radiotracer for Serotonin 5-HT6 Receptors , 2017, Front. Pharmacol..

[8]  W. Kummer,et al.  Caveolin-1: Functional Insights into Its Role in Muscarine- and Serotonin-Induced Smooth Muscle Constriction in Murine Airways , 2017, Front. Physiol..

[9]  A. Meneses.  Neural activity, memory, and dementias: serotonergic markers , 2017, Behavioural pharmacology.

[10]  V. Bouet,et al.  Therapeutic Potential of 5-HT6 Receptor Agonists. , 2015, Journal of medicinal chemistry.

[11]  L. Tremblay,et al.  Preclinical evaluation of [18F]2FNQ1P as the first fluorinated serotonin 5-HT6 radioligand for PET imaging , 2015, European Journal of Nuclear Medicine and Molecular Imaging.

[12]  W. Cai.  Positron emission tomography: state of the art. , 2014, Molecular pharmaceutics.

[13]  V. Bouet,et al.  5-HT6 receptor antagonists as treatment for age-related cognitive decline , 2014, Reviews in the neurosciences.

[14]  Hao Hong,et al.  Positron Emission Tomography Image-Guided Drug Delivery: Current Status and Future Perspectives , 2014, Molecular pharmaceutics.

[15]  M. Lai,et al.  Serotonergic Therapies for Cognitive Symptoms in Alzheimer’s Disease: Rationale and Current Status , 2014, Drugs.

[16]  L. Zimmer,et al.  Syntheses, radiolabelings, and in vitro evaluations of fluorinated PET radioligands of 5-HT6 serotoninergic receptors. , 2014, Journal of medicinal chemistry.

[17]  F. Bordi,et al.  Serotonin receptor of type 6 (5-HT6) in human prefrontal cortex and hippocampus post-mortem: An immunohistochemical and immunofluorescence study , 2013, Neurochemistry International.

[18]  S. O’Mara,et al.  Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457 , 2012, Neuropharmacology.

[19]  A. Luxen,et al.  PET radiotracers for molecular imaging in the brain: Past, present and future , 2012, NeuroImage.

[20]  A. Chopra.  [11C]-[N-Methyl]3-[(3-fluorophenyl)sulfonyl]-8-(4-methyl-1-piperazinyl)quinoline , 2012 .

[21]  C. Christoffersen,et al.  Characterization of [³H]Lu AE60157 ([³H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine₆ (5-HT₆) receptors in vivo. , 2012, European journal of pharmacology.

[22]  Steen Jakobsen,et al.  Radiosynthesis and Characterization of 11C-GSK215083 as a PET Radioligand for the 5-HT6 Receptor , 2012, The Journal of Nuclear Medicine.

[23]  F. Bordi,et al.  Distribution of Serotonin Receptor of Type 6 (5-HT6) in Human Brain Post-mortem. A Pharmacology, Autoradiography and Immunohistochemistry Study , 2012, Neurochemical Research.

[24]  R. Parsey,et al.  Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide as an imaging probe for 5-HT6 receptors. , 2011, Bioorganic & medicinal chemistry.

[25]  Oliver Langer,et al.  Approaches using molecular imaging technology -- use of PET in clinical microdose studies. , 2011, Advanced drug delivery reviews.

[26]  Ben Grayson,et al.  Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. , 2010, The international journal of neuropsychopharmacology.

[27]  B. Roth,et al.  The expanded biology of serotonin. , 2009, Annual review of medicine.

[28]  A. Luxen,et al.  Cyclosporine, a P-glycoprotein modulator, increases [18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies , 2008, European Journal of Nuclear Medicine and Molecular Imaging.

[29]  J. Willmann,et al.  Molecular imaging in drug development , 2008, Nature Reviews Drug Discovery.

[30]  Pius August Schubiger,et al.  Molecular imaging with PET. , 2008, Chemical reviews.

[31]  D. Le Bars,et al.  Synthesis and biological evaluation in rat and cat of [18F]12ST05 as a potential 5-HT6 PET radioligand. , 2007, Nuclear medicine and biology.

[32]  C. Marsden,et al.  5-ht6 receptors. , 2004, Current drug targets. CNS and neurological disorders.

[33]  Paul J. Harrison,et al.  5‐HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: Autoradiographic studies with [125I]SB‐258585 , 2002, Synapse.

[34]  R. Leahy,et al.  Whole-body skeletal imaging in mice utilizing microPET: optimization of reproducibility and applications in animal models of bone disease , 2002, European Journal of Nuclear Medicine and Molecular Imaging.

[35]  D. Middlemiss,et al.  Characterization of [125I]‐SB‐258585 binding to human recombinant and native 5‐HT6 receptors in rat, pig and human brain tissue , 2000 .

[36]  A. Sleight,et al.  The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. , 1998, Molecular pharmacology.

[37]  D. Sibley,et al.  Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor , 1996, Journal of neurochemistry.

[38]  J. Schwartz,et al.  A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. , 1993, Biochemical and biophysical research communications.

[39]  D. Sibley,et al.  Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. , 1993, Molecular pharmacology.

[40]  Alun G. Jones,et al.  Interspecies variation in biodistribution of technetium (2-carbomethoxy-2-isocyanopropane)6+. , 1992, Journal of nuclear medicine : official publication, Society of Nuclear Medicine.

[41]  T. Billard,et al.  Serotonin receptor imaging by 18F-PET , 2019, Fluorine in Life Sciences: Pharmaceuticals, Medicinal Diagnostics, and Agrochemicals.

[42]  J. Gosden,et al.  The 5-HT6 receptor as a target for developing novel antiobesity drugs. , 2011, International review of neurobiology.

[43]  E. Mitchell.  5-HT6 receptor ligands as antidementia drugs. , 2011, International review of neurobiology.

[44]  A. Meneses,et al.  5-HT6 receptor memory and amnesia: behavioral pharmacology--learning and memory processes. , 2011, International review of neurobiology.

[45]  M. Blau,et al.  18 F-fluoride for bone imaging. , 1972, Seminars in nuclear medicine.