Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.
暂无分享,去创建一个
[1] Greg A. Hostetler,et al. In Search of Potent 5‐HT6 Receptor Inverse Agonists , 2014, Chemical biology & drug design.
[2] Karla K Kopec,et al. Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists. , 2014, Bioorganic & medicinal chemistry letters.
[3] Craig W Lindsley,et al. Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease. , 2013, Drug discovery today.
[4] R. Stevens,et al. Structural Features for Functional Selectivity at Serotonin Receptors , 2013, Science.
[5] D. Le Bars,et al. Current status of positron emission tomography radiotracers for serotonin receptors in humans. , 2013, Journal of labelled compounds & radiopharmaceuticals.
[6] A. A. Ivanenkov. Small Molecule 5-HT6R Ligands: A Comprehensive Insight into their Selectivity and Activity , 2013 .
[7] M. Babu,et al. Molecular signatures of G-protein-coupled receptors , 2013, Nature.
[8] R. Nirogi,et al. Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N₁-arylsulfonyl indole derivatives as 5-HT₆ receptor ligands. , 2012, Bioorganic & medicinal chemistry letters.
[9] R. Nirogi,et al. Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT₆ receptor antagonists. , 2012, Journal of medicinal chemistry.
[10] Alan A. Wilson,et al. Biodistribution and Radiation Dosimetry of the Serotonin 5-HT6 Ligand [11C]GSK215083 Determined from Human Whole-Body PET , 2012, Molecular Imaging and Biology.
[11] Y. Ivanenkov,et al. 5HT6 receptor antagonists: a patent update. Part 1. Sulfonyl derivatives , 2012, Expert opinion on therapeutic patents.
[12] A. Verkhratsky,et al. The serotonergic system in ageing and Alzheimer's disease , 2012, Progress in Neurobiology.
[13] I. Okun,et al. Antagonists of 5-HT₆ receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines-Synthesis and 'structure-activity' relationship. , 2012, Bioorganic & medicinal chemistry letters.
[14] Ying Xia,et al. Neurotransmitter receptors and cognitive dysfunction in Alzheimer's disease and Parkinson's disease , 2012, Progress in Neurobiology.
[15] K. Nacro,et al. Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists. , 2012, Bioorganic & medicinal chemistry letters.
[16] Karla K Kopec,et al. Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. , 2012, Bioorganic & medicinal chemistry letters.
[17] S. Tkachenko,et al. Synthesis and structure-activity relationship (SAR) of (5,7-disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as potent serotonin 5-HT(6) receptor (5-HT(6)R) antagonists. , 2011, Journal of medicinal chemistry.
[18] H. Parri,et al. Research update: Alpha7 nicotinic acetylcholine receptor mechanisms in Alzheimer's disease. , 2011, Biochemical pharmacology.
[19] N. Herrmann,et al. The Role of Dopamine in Symptoms and Treatment of Apathy in Alzheimer's Disease , 2011, CNS neuroscience & therapeutics.
[20] J. Venhorst,et al. N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT₆R) antagonists with unique structural features. , 2011, Journal of medicinal chemistry.
[21] J. Venhorst,et al. Two novel 5-HT6 receptor antagonists ameliorate scopolamine-induced memory deficits in the object recognition and object location tasks in Wistar rats , 2011, Neurobiology of Learning and Memory.
[22] W. Geldenhuys,et al. Role of Serotonin in Alzheimer’s Disease , 2011, CNS drugs.
[23] A. Terry,et al. Alzheimer's disease and age-related memory decline (preclinical) , 2011, Pharmacology Biochemistry and Behavior.
[24] M. Gold,et al. SB‐742457 and donepezil in Alzheimer disease: a randomized, placebo‐controlled study , 2011, International journal of geriatric psychiatry.
[25] F. Bordi,et al. 5-HT6 pharmacology inconsistencies , 2011, Pharmacology Biochemistry and Behavior.
[26] S. Tkachenko,et al. 2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: new series of highly potent and specific serotonin 5-HT6 receptor antagonists. , 2011, European journal of medicinal chemistry.
[27] A. Palmer,et al. Neuroprotective therapeutics for Alzheimer's disease: progress and prospects. , 2011, Trends in pharmacological sciences.
[28] M. Ramírez,et al. 5-HT(6) receptor and cognition. , 2011, Current opinion in pharmacology.
[29] L. Tan,et al. Roles of β-adrenergic receptors in Alzheimer's disease: Implications for novel therapeutics , 2011, Brain Research Bulletin.
[30] T. Comery,et al. 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. , 2010, Journal of medicinal chemistry.
[31] M. Carter,et al. The Development of New Therapeutics for Alzheimer's Disease , 2010, Clinical pharmacology and therapeutics.
[32] J. A. González-Vera,et al. Development of molecular probes for the human 5-HT(6) receptor. , 2010, Journal of medicinal chemistry.
[33] 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.
[34] F. LaFerla. Pathways linking Abeta and tau pathologies. , 2010, Biochemical Society transactions.
[35] M. Gold,et al. Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's disease. , 2010, Current Alzheimer research.
[36] M. Solas,et al. Signalling pathways associated with 5-HT6 receptors: relevance for cognitive effects. , 2010, The international journal of neuropsychopharmacology.
[37] A. Wesołowska. Potential role of the 5-HT_6 receptor in depression and anxiety: an overview of preclinical data , 2010, Pharmacological reports : PR.
[38] B. Winblad,et al. Alzheimer's disease: clinical trials and drug development , 2010, The Lancet Neurology.
[39] S. Tkachenko,et al. (3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor. , 2010, Journal of medicinal chemistry.
[40] B. Roth,et al. The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs. , 2010, Current topics in medicinal chemistry.
[41] Jessica Sallander,et al. Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation. , 2010, Journal of medicinal chemistry.
[42] C. González-Espinosa,et al. Time-course of 5-HT6 receptor mRNA expression during memory consolidation and amnesia , 2010, Neurobiology of Learning and Memory.
[43] G. Rosse,et al. 5-HT6 receptor antagonists as potential therapeutics for cognitive impairment. , 2010, Current topics in medicinal chemistry.
[44] John Dunlop,et al. Neuronal nicotinic acetylcholine receptors - targets for the development of drugs to treat cognitive impairment associated with schizophrenia and Alzheimer's disease. , 2010, Current topics in medicinal chemistry.
[45] V. R. Marcy,et al. Activation of the 5-HT6 receptor attenuates long-term potentiation and facilitates GABAergic neurotransmission in rat hippocampus , 2009, Neuroscience.
[46] Christina A. Wilson,et al. Enhancing cognition in neurologic disorders: Potential usefulness of 5-HT6 antagonists , 2009, Drugs of the Future.
[47] Michael J Marino,et al. Dimebolin is a 5-HT6 antagonist with acute cognition enhancing activities. , 2009, Biochemical pharmacology.
[48] J. Holenz,et al. Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. , 2009, Journal of medicinal chemistry.
[49] W. Geldenhuys,et al. The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer’s disease , 2009, Expert review of neurotherapeutics.
[50] L. W. Cooke,et al. Synthesis and SAR of tolylamine 5-HT6 antagonists. , 2009, Bioorganic & medicinal chemistry letters.
[51] A. Robichaud,et al. 5‐HT6 antagonists as potential treatment for cognitive dysfunction , 2009 .
[52] David B. Sattelle,et al. Nicotinic Acetylcholine Receptor Signalling: Roles in Alzheimer's Disease and Amyloid Neuroprotection , 2009, Pharmacological Reviews.
[53] M. Shahid,et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature , 2009, Journal of psychopharmacology.
[54] K. Fone. An update on the role of the 5-hydroxytryptamine6 receptor in cognitive function , 2008, Neuropharmacology.
[55] F. Gil-Bea,et al. Effects of 5‐HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat , 2008, British journal of pharmacology.
[56] Charles A. Marsden,et al. A role for the 5-HT1A, 5-HT4 and 5-HT6 receptors in learning and memory , 2008 .
[57] W. Geldenhuys,et al. Serotonin 5-HT6 receptor antagonists for the treatment of Alzheimer's disease. , 2008, Current topics in medicinal chemistry.
[58] M. Sano,et al. Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study , 2008, The Lancet.
[59] T. Comery,et al. A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. , 2008, Bioorganic & medicinal chemistry letters.
[60] Neil Upton,et al. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer’s disease , 2008, Neurotherapeutics.
[61] Derek Cole,et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466 , 2008, Neuropsychopharmacology.
[62] X. Codony,et al. Selective 5-HT6 receptor ligands: progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders. , 2008, Pharmacology & therapeutics.
[63] B. Roth,et al. Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. , 2008, Journal of medicinal chemistry.
[64] Jae Yang Kong,et al. Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. , 2008, Bioorganic & medicinal chemistry letters.
[65] G. Bernardi,et al. Endogenous Serotonin Excites Striatal Cholinergic Interneurons via the Activation of 5-HT 2C, 5-HT6, and 5-HT7 Serotonin Receptors: Implications for Extrapyramidal Side Effects of Serotonin Reuptake Inhibitors , 2007, Neuropsychopharmacology.
[66] J. Neumaier,et al. Increased Expression of 5-HT6 Receptors in the Rat Dorsomedial Striatum Impairs Instrumental Learning , 2007, Neuropsychopharmacology.
[67] D. Misner,et al. 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists. , 2007, Bioorganic & medicinal chemistry letters.
[68] R. Schreiber,et al. Effects of the novel 5-HT6 receptor antagonist RO4368554 in rat models for cognition and sensorimotor gating , 2007, European Neuropsychopharmacology.
[69] J. Baik,et al. The Novel Cellular Mechanism of Human 5-HT6 Receptor through an Interaction with Fyn* , 2007, Journal of Biological Chemistry.
[70] C. Regan,et al. SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. , 2006, European journal of pharmacology.
[71] B. Roth,et al. Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. , 2006, Bioorganic & medicinal chemistry letters.
[72] M. Garcia-Alloza,et al. Lack of localization of 5‐HT6 receptors on cholinergic neurons: implication of multiple neurotransmitter systems in 5‐HT6 receptor‐mediated acetylcholine release , 2006, The European journal of neuroscience.
[73] B. Roth,et al. Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. , 2006, Journal of medicinal chemistry.
[74] J. Holenz,et al. Medicinal chemistry strategies to 5-HT(6) receptor ligands as potential cognitive enhancers and antiobesity agents. , 2006, Drug discovery today.
[75] J. Neumaier,et al. 5-HT6 receptors: a novel target for cognitive enhancement. , 2005, Pharmacology & therapeutics.
[76] Michael A. Briggs,et al. Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists. , 2005, Bioorganic & medicinal chemistry letters.
[77] A. Meneses,et al. Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task , 2005, Pharmacology Biochemistry and Behavior.
[78] Leonardo Pardo,et al. A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists. , 2005, Journal of medicinal chemistry.
[79] V. Brown,et al. 5-HT6 receptor antagonists improve performance in an attentional set shifting task in rats , 2005, Psychopharmacology.
[80] J. Holenz,et al. Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. , 2005, Journal of medicinal chemistry.
[81] V. Setola,et al. 1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. , 2005, Bioorganic & medicinal chemistry letters.
[82] J. Ellingboe,et al. Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. , 2005, Journal of medicinal chemistry.
[83] J. Ellingboe,et al. N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. , 2005, Bioorganic & medicinal chemistry letters.
[84] R. Glennon,et al. Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. , 2004, Bioorganic & medicinal chemistry letters.
[85] A. Sleight,et al. 5-HT6 receptor antagonists reverse delay-dependent deficits in novel object discrimination by enhancing consolidation—an effect sensitive to NMDA receptor antagonism , 2004, Neuropharmacology.
[86] J. Standridge. Pharmacotherapeutic approaches to the treatment of Alzheimer's disease. , 2004, Clinical therapeutics.
[87] M. Garcia-Alloza,et al. Differential Involvement of 5-HT1B/1D and 5-HT6 Receptors in Cognitive and Non-cognitive Symptoms in Alzheimer's Disease , 2004, Neuropsychopharmacology.
[88] C. Marsden,et al. 5-ht6 receptors. , 2004, Current drug targets. CNS and neurological disorders.
[89] V. Setola,et al. Why mice are neither miniature humans nor small rats: a cautionary tale involving 5-hydroxytryptamine-6 serotonin receptor species variants. , 2003, Molecular pharmacology.
[90] G. W. Price,et al. Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling. , 2003, Molecular pharmacology.
[91] V. Gribkoff,et al. An Assessment of the Effects of Serotonin 6 (5-HT6) Receptor Antagonists in Rodent Models of Learning , 2003, Journal of Pharmacology and Experimental Therapeutics.
[92] A. Sleight,et al. Reversal of a cholinergic-induced deficit in a rodent model of recognition memory by the selective 5-HT6 receptor antagonist, Ro 04-6790 , 2003, Psychopharmacology.
[93] S. Nawoschik,et al. Characterization of the 5-HT6 receptor coupled to Ca2+ signaling using an enabling chimeric G-protein. , 2003, European journal of pharmacology.
[94] T. Myhrer. Neurotransmitter systems involved in learning and memory in the rat: a meta-analysis based on studies of four behavioral tasks , 2003, Brain Research Reviews.
[95] M. Bös,et al. Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist. , 2003, Journal of medicinal chemistry.
[96] G. Bernardi,et al. Association study of the 5-hydroxytryptamine6 receptor gene in Alzheimer's disease , 2002, Neuroscience Letters.
[97] R. Dias,et al. Memories are made of this (perhaps): a review of serotonin 5-HT(6) receptor ligands and their biological functions. , 2002, Current topics in medicinal chemistry.
[98] S. Bromidge,et al. Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists. , 2002, Bioorganic & medicinal chemistry letters.
[99] A. Slassi,et al. Recent progress in 5-HT6 receptor antagonists for the treatment of CNS diseases , 2002 .
[100] J. Hagan,et al. 5-HT6 receptor antagonists enhance retention of a water maze task in the rat , 2001, Psychopharmacology.
[101] L. Dawson,et al. The 5-HT6 Receptor Antagonist SB-271046 Selectively Enhances Excitatory Neurotransmission in the Rat Frontal Cortex and Hippocampus , 2001, Neuropsychopharmacology.
[102] M. Knowles,et al. N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. , 2001, Journal of medicinal chemistry.
[103] A. Sleight,et al. A role for 5-ht6 receptors in retention of spatial learning in the Morris water maze , 2001, Neuropharmacology.
[104] A. Meneses. Effects of the 5-HT6 receptor antagonist Ro 04-6790 on learning consolidation , 2001, Behavioural Brain Research.
[105] S. Bromidge,et al. Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134). , 2001, Bioorganic & medicinal chemistry letters.
[106] B. Roth,et al. N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. , 2000, Bioorganic & medicinal chemistry letters.
[107] D. Middlemiss,et al. Characterization of SB‐271046: A potent, selective and orally active 5‐HT6 receptor antagonist , 2000, British journal of pharmacology.
[108] 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 .
[109] B. Roth,et al. 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. , 2000, Journal of medicinal chemistry.
[110] S. Tsai,et al. Association analysis of the 5-HT6 receptor polymorphism C267T in Alzheimer's disease , 1999, Neuroscience Letters.
[111] A. Brown,et al. 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. , 1999, Journal of medicinal chemistry.
[112] F. Monsma,et al. Identification of Residues in Transmembrane Regions III and VI that Contribute to the Ligand Binding Site of the Serotonin 5‐HT6 Receptor , 1998, Journal of neurochemistry.
[113] A. Sleight,et al. Characterization of Ro 04‐6790 and Ro 63‐0563: potent and selective antagonists at human and rat 5‐HT6 receptors , 1998, British journal of pharmacology.
[114] F. Monsma,et al. Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. , 1997, Molecular pharmacology.
[115] L. Lanfumey,et al. Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system , 1997, Brain Research.
[116] M. Martres,et al. Quantitative RT‐PCR distribution of serotonin 5‐HT6 receptor mRNA in the central nervous system of control or 5,7‐dihydroxytryptamine‐treated rats , 1996, Synapse.
[117] D. Sibley,et al. Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor , 1996, Journal of neurochemistry.
[118] F. Monsma,et al. Determination of the role of the 5-ht6 receptor in the rat brain: a study using antisense oligonucleotides. , 1995, The Journal of pharmacology and experimental therapeutics.
[119] J. Bockaert,et al. 5-HT6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture. , 1994, Neuroreport.
[120] D. Sibley,et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. , 1994, The Journal of pharmacology and experimental therapeutics.
[121] 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.
[122] D. Sibley,et al. Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. , 1993, Molecular pharmacology.
[123] D. Marazziti,et al. Serotonin receptors of type 6 (5-HT6): from neuroscience to clinical pharmacology. , 2013, Current medicinal chemistry.
[124] A. Meneses,et al. 5-HT6 receptor memory and amnesia: behavioral pharmacology--learning and memory processes. , 2011, International review of neurobiology.
[125] A. Robichaud,et al. 5-HT6 medicinal chemistry. , 2010, International review of neurobiology.
[126] Hyunah Choo,et al. New Serotonin 5-HT6 Ligands from Common Feature Pharmacophore Hypotheses , 2008, J. Chem. Inf. Model..
[127] X. Guitart,et al. Drug discovery targets: 5-HT6 receptor , 2005 .
[128] K. J. Murphy,et al. The 5-HT6 Receptor Antagonist SB-271046 Reverses Scopolamine-Disrupted Consolidation of a Passive Avoidance Task and Ameliorates Spatial Task Deficits in Aged Rats , 2004, Neuropsychopharmacology.
[129] P. Scheltens,et al. Treatment of Alzheimer's disease: current status and new perspectives. , 2003, The Lancet. Neurology.