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

Berger, 2009, The expanded biology of serotonin, Annu Rev Med, 60, 355, 10.1146/annurev.med.60.042307.110802 Monsma, 1993, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs, Mol Pharmacol, 43, 320 Ruat, 1993, A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation, Biochem Biophys Res Commun, 193, 268, 10.1006/bbrc.1993.1619 Kohen, 1996, Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor, J Neurochem, 66, 47, 10.1046/j.1471-4159.1996.66010047.x Mitchell, 2011, 5-HT6 receptor ligands as antidementia drugs, Int Rev Neurobiol, 96, 163, 10.1016/B978-0-12-385902-0.00007-3 Quiedeville, 2014, 5-HT6 receptor antagonists as treatment for age-related cognitive decline, Rev Neurosci, 25, 417, 10.1515/revneuro-2014-0013 Heal, 2011, The 5-HT6 receptor as a target for developing novel antiobesity drugs, Int Rev Neurobiol, 96, 73, 10.1016/B978-0-12-385902-0.00004-8 Kotańska, 2018, Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating, Metab Brain Dis, 33, 733, 10.1007/s11011-017-0175-1 Marazziti, 2012, Distribution of serotonin receptor of type 6 (5-HT₆) in human brain post-mortem. A pharmacology, autoradiography and immunohistochemistry study, Neurochem Res, 37, 920, 10.1007/s11064-011-0684-y Marazziti, 2013, Serotonin receptor of type 6 (5-HT6) in human prefrontal cortex and hippocampus post-mortem: an immunohistochemical and immunofluorescence study, Neurochem Int, 62, 182, 10.1016/j.neuint.2012.11.013 Ramirez, 2014, Serotonergic therapies for cognitive symptoms in Alzheimer’s disease: rationale and current status, Drugs, 74, 729, 10.1007/s40265-014-0217-5 Meneses, 2011, 5-HT6 receptor memory and amnesia: behavioral pharmacology—learning and memory processes, Int Rev Neurobiol, 96, 27, 10.1016/B978-0-12-385902-0.00002-4 Arnt, 2010, Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats, Int J Neuropsychopharmacol, 13, 1021, 10.1017/S1461145710000659 Callaghan, 2012, Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457, Neuropharmacology, 63, 890, 10.1016/j.neuropharm.2012.06.034 Bennett, 2018, Lack of benefit with idalopirdine for Alzheimer disease: another therapeutic failure in a complex disease process, JAMA, 319, 123, 10.1001/jama.2017.19700 Fullerton, 2018, 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, Alzheimers Res Ther, 10, 38, 10.1186/s13195-018-0368-9 Nirogi, 2019, SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization, Behav Pharmacol, 30, 16, 10.1097/FBP.0000000000000414 Vanda, 2018, Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties, Eur J Med Chem, 144, 716, 10.1016/j.ejmech.2017.12.053 Karila, 2015, Therapeutic potential of 5-HT6 receptor agonists, J Med Chem, 58, 7901, 10.1021/acs.jmedchem.5b00179 Zimmer, 2012, PET radiotracers for molecular imaging in the brain: past, present and future, Neuroimage, 61, 363, 10.1016/j.neuroimage.2011.12.037 Cai, 2014, Positron emission tomography: state of the art, Mol Pharm, 11, 3773, 10.1021/mp5005383 Ametamey, 2008, Molecular imaging with PET, Chem Rev, 108, 1501, 10.1021/cr0782426 Sgambato-Faure, 2017, Characterization and reliability of [18F]2FNQ1P in cynomolgus monkeys as a PET radiotracer for serotonin 5-HT6 receptors, Front Pharmacol, 8, 471, 10.3389/fphar.2017.00471 Wagner, 2011, Approaches using molecular imaging technology — use of PET in clinical microdose studies, Adv Drug Deliv Rev, 63, 539, 10.1016/j.addr.2010.09.011 Chakravarty, 2014, Positron emission tomography image-guided drug delivery: current status and future perspectives, Mol Pharm, 11, 3777, 10.1021/mp500173s Willmann, 2008, Molecular imaging in drug development, Nat Rev Drug Discov, 7, 591, 10.1038/nrd2290 Tang, 2007, Synthesis and biological evaluation in rat and cat of [18F]12ST05 as a potential 5-HT6 PET radioligand, Nucl Med Biol, 34, 995, 10.1016/j.nucmedbio.2007.07.002 Parker, 2012, Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor, J Nucl Med, 53, 295, 10.2967/jnumed.111.093419 Liu, 2011, 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, Bioorg Med Chem, 19, 5255, 10.1016/j.bmc.2011.06.090 Billard, 2019, Serotonin receptor imaging by 18F-PET, 459 Meneses, 2017, Neural activity, memory, and dementias: serotonergic markers, Behav Pharmacol, 28, 132, 10.1097/FBP.0000000000000279 Colomb, 2014, Syntheses, radiolabelings, and in vitro evaluations of fluorinated PET radioligands of 5-HT6 serotoninergic receptors, J Med Chem, 57, 3884, 10.1021/jm500372e Becker, 2015, Preclinical evaluation of [18F]2FNQ1P as the first fluorinated serotonin 5-HT6 radioligand for PET imaging, Eur J Nucl Med Mol Imaging, 42, 495, 10.1007/s00259-014-2936-y Kronauge, 1992, Interspecies variation in biodistribution of technetium (2-carbomethoxy-2-isocyanopropane)6+, J Nucl Med, 33, 1357 Chopra, 2004, [11C]-[N-methyl]3-[(3-fluorophenyl)sulfonyl]-8-(4-methyl-1-piperazinyl)quinoline Witten, 2012, Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine₆ (5-HT₆) receptors in vivo, Eur J Pharmacol, 676, 6, 10.1016/j.ejphar.2011.11.029 East, 2002, 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585, Synapse, 45, 191, 10.1002/syn.10097 Hirst, 2000, Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue, Br J Pharmacol, 130, 1597, 10.1038/sj.bjp.0703458 Boess, 1998, The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum, Mol Pharmacol, 54, 577, 10.1124/mol.54.3.577 Woolley, 2004, 5-ht6 receptors, Curr Drug Targets CNS Neurol Disord, 3, 59, 10.2174/1568007043482561 Laćan, 2008, Cyclosporine, a P-glycoprotein modulator, increases [18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies, Eur J Nucl Med Mol Imaging, 35, 2256, 10.1007/s00259-008-0832-z Berger, 2002, Whole-body skeletal imaging in mice utilizing microPET: optimization of reproducibility and applications in animal models of bone disease, Eur J Nucl Med Mol Imaging, 29, 1225, 10.1007/s00259-002-0850-1 Blau, 1972, 18 F-fluoride for bone imaging, Semin Nucl Med, 2, 31, 10.1016/S0001-2998(72)80005-9 Keshavarz, 2017, Caveolin-1: functional insights into its role in muscarine- and serotonin-induced smooth muscle constriction in murine airways, Front Physiol, 8, 295, 10.3389/fphys.2017.00295 Khoury, 2018, The role of 5 HT6-receptor antagonists in Alzheimer’s disease: an update, Expert Opin Investig Drugs, 27, 523, 10.1080/13543784.2018.1483334