Serotonin 5-HT6 Receptor Antagonists in Alzheimer’s Disease: Therapeutic Rationale and Current Development Status

Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT 6 receptor antagonists. Design, synthesis and biological evaluation

(2016) Anna Więckowska et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT 4 R) partial agonist and 5-HT 6 R antagonist activities, as potential treatment of Alzheimer’s disease

(2016) Samir Yahiaoui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders

(2016) Alexandre V. Ivachtchenko et al.   JOURNAL OF ALZHEIMERS DISEASE

Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation

(2016) Gonzalo Vera et al.   MOLECULES

The selective 5-HT 6 receptor antagonist SLV has putative cognitive- and social interaction enhancing properties in rodent models of cognitive impairment

(2016) N.M.W.J. de Bruin et al.   NEUROBIOLOGY OF LEARNING AND MEMORY

N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties

(2016) Paweł Zajdel et al.   ACS Medicinal Chemistry Letters

3D QSAR, pharmacophore and molecular docking studies of known inhibitors and designing of novel inhibitors for M18 aspartyl aminopeptidase of Plasmodium falciparum

(2016) Madhulata Kumari et al.   BMC STRUCTURAL BIOLOGY

Disturbed Neurotransmitter Transporter Expression in Alzheimer’s Disease Brain

(2016) Kevin H. Chen et al.   JOURNAL OF ALZHEIMERS DISEASE

Pharmacological Evidence for 5-HT6 Receptor Modulation of 5-HT Neuron Firing in Vivo

(2015) Julia T. Brouard et al.   ACS Chemical Neuroscience

Investigational drugs targeting 5-HT6 receptors for the treatment of Alzheimer’s disease

(2015) Karsten Wicke et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Distribution of serotonin receptor 5-HT6 mRNA in rat neuronal subpopulations: A double in situ hybridization study

(2015) L. Helboe et al.   NEUROSCIENCE

5-HT6 receptor agonism facilitates emotional learning

(2015) Marcela Pereira et al.   Frontiers in Pharmacology

Serotonin, neural markers, and memory

(2015) Alfredo Meneses   Frontiers in Pharmacology

Enhancing cognition in neurologic disorders: Potential usefulness of 5-HT6 antagonists

(2015) C. Wilson et al.   DRUGS OF THE FUTURE

A CLINICAL POSITRON EMISSION TOMOGRAPHY (PET) STUDY INVESTIGATING OCCUPANCY AT THE 5-HT6 RECEPTOR AFTER MULTIPLE ORAL DOSES OF LU AE58054 TO HEALTHY MEN

(2014) Ellen Schmidt et al.   Alzheimers & Dementia

DISTRIBUTION OF SEROTONIN RECEPTOR 5-HT6 MRNA IN SELECTED NEURONAL POPULATIONS IN RAT BRAIN: A DOUBLE-LABELLING IN SITU HYBRIDIZATION STUDY

(2014) Inge de Jong et al.   Alzheimers & Dementia

Preclinical evaluation of [18F]2FNQ1P as the first fluorinated serotonin 5-HT6 radioligand for PET imaging

(2014) Guillaume Becker et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Serotonin 5-HT6 Receptor Antagonists for the Treatment of Cognitive Deficiency in Alzheimer’s Disease

(2014) Bellinda Benhamú et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological evaluation of the anxiolytic-like effects of EMD 386088, a partial 5-HT6 receptor agonist, in the rat elevated plus-maze and Vogel conflict tests

(2014) Magdalena Jastrzębska-Więsek et al.   NEUROPHARMACOLOGY

Partial agonist efficacy of EMD386088, a 5-HT6 receptor ligand, in functional in vitro assays

(2014) Magdalena Jastrzębska-Więsek et al.   Pharmacological Reports

The procognitive effects of 5-HT6 receptor ligands in animal models of schizophrenia

(2014) Agnieszka Nikiforuk   REVIEWS IN THE NEUROSCIENCES

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

5HT6receptor antagonists: a patent update. Part 1. Sulfonyl derivatives

(2012) Alexandre V Ivachtchenko et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

5-HT6receptor modulators: a patent update. Part 2. Diversity in heterocyclic scaffolds

(2012) Alexandre V Ivachtchenko et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

5-HT6 receptor blockade differentially affects scopolamine-induced deficits of working memory, recognition memory and aversive learning in mice

(2012) Virginie Da Silva Costa-Aze et al.   PSYCHOPHARMACOLOGY

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) Fei Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

5-HT6 receptor and cognition

(2011) Xabier Codony et al.   CURRENT OPINION IN PHARMACOLOGY

ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors

(2011) Teresa Riccioni et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo

(2011) Louise Witten et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

N′-(Arylsulfonyl)pyrazoline-1-carboxamidines as Novel, Neutral 5-Hydroxytryptamine 6 Receptor (5-HT6R) Antagonists with Unique Structural Features

(2011) Arnold van Loevezijn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biodistribution and Radiation Dosimetry of the Serotonin 5-HT6 Ligand [11C]GSK215083 Determined from Human Whole-Body PET

(2011) Robert A. Comley et al.   MOLECULAR IMAGING AND BIOLOGY

Two novel 5-HT6 receptor antagonists ameliorate scopolamine-induced memory deficits in the object recognition and object location tasks in Wistar rats

(2011) N.M.W.J. de Bruin et al.   NEUROBIOLOGY OF LEARNING AND MEMORY

Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission

(2011) Annalisa Tassone et al.   NEUROPHARMACOLOGY

The 5-HT6 receptor agonist EMD 386088 produces antidepressant and anxiolytic effects in rats after intrahippocampal administration

(2011) Agnieszka Nikiforuk et al.   PSYCHOPHARMACOLOGY

5-HT6 receptor ligands, EMD386088 and SB258585, differentially regulate 5-HT6 receptor-independent events

(2011) Hyung-Mun Yun et al.   TOXICOLOGY IN VITRO

Safety, tolerability, and preliminary efficacy of SAM-531, a 5HT-6 antagonist, in subjects with mild-to-moderate Alzheimer's disease: Results from a phase 2a study

(2010) Claudine Brisard et al.   Alzheimers & Dementia

5-HT6 Receptor Antagonists as Potential Therapeutics for Cognitive Impairment

(2010) Gerard Rosse et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

5-hydroxytryptamine subtype 6 receptor modulators: a patent survey

(2010) Alexandre V Ivachtchenko et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats

(2010) Jorn Arnt et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Physical Interaction of Jab1 with Human Serotonin 6 G-protein-coupled Receptor and Their Possible Roles in Cell Survival

(2010) Hyung-Mun Yun et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Alzheimer's Disease

(2010) Henry W. Querfurth et al.   NEW ENGLAND JOURNAL OF MEDICINE

E-6801, a 5-HT6 receptor agonist, improves recognition memory by combined modulation of cholinergic and glutamatergic neurotransmission in the rat

(2010) Ian Kendall et al.   PSYCHOPHARMACOLOGY

Antidepressant and anxiolytic effects of selective 5-HT6 receptor agonists in rats

(2010) Gregory V. Carr et al.   PSYCHOPHARMACOLOGY

Dimebon disappointment

(2010) Roy W Jones   Alzheimers Research & Therapy

Signalling pathways associated with 5-HT6 receptors: relevance for cognitive effects

(2009) Beatriz Marcos et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Procognitive 5-HT6 antagonists in the rat forced swimming test: Potential therapeutic utility in mood disorders associated with Alzheimer's disease

(2009) Kazufumi Hirano et al.   LIFE SCIENCES

Time-course of 5-HT6 receptor mRNA expression during memory consolidation and amnesia

(2009) A. Huerta-Rivas et al.   NEUROBIOLOGY OF LEARNING AND MEMORY

In silico modeling system: A national research resource for simulation of complex brain disorders

(2008) Zaven S. Khachaturian et al.   Alzheimers & Dementia

Genomic analysis of serotonin receptors in learning and memory

(2008) Sebastiano Cavallaro   BEHAVIOURAL BRAIN RESEARCH

Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat

(2008) B Marcos et al.   BRITISH JOURNAL OF PHARMACOLOGY

Actions of novel agonists, antagonists and antipsychotic agents at recombinant rat 5-HT6 receptors: A comparative study of coupling to Gαs

(2008) Delphine S. Dupuis et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

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) Rachelle S Doody et al.   LANCET

The selective 5-HT6 receptor antagonists SB-271046 and SB-399885 potentiate NCAM PSA immunolabeling of dentate granule cells, but not neurogenesis, in the hippocampal formation of mature Wistar rats

(2008) A FOLEY et al.   NEUROPHARMACOLOGY

An update on the role of the 5-hydroxytryptamine6 receptor in cognitive function

(2008) Kevin C.F. Fone   NEUROPHARMACOLOGY

5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer’s disease

(2008) Neil Upton et al.   Neurotherapeutics

A role for the 5-HT1A, 5-HT4 and 5-HT6 receptors in learning and memory

(2008) M KING et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Selective 5-HT6 receptor ligands: Progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders

(2007) D.J. Heal et al.   PHARMACOLOGY & THERAPEUTICS