Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders

Towards in vivo imaging of functionally active 5-HT1A receptors in schizophrenia: concepts and challenges

(2021) Oriane Razakarivony et al.   Translational Psychiatry

The Roles of Serotonin in Neuropsychiatric Disorders

(2021) Mahsa Pourhamzeh et al.   CELLULAR AND MOLECULAR NEUROBIOLOGY

The Role of Central Serotonin Neurons and 5-HT Heteroreceptor Complexes in the Pathophysiology of Depression: A Historical Perspective and Future Prospects

(2021) Dasiel O. Borroto-Escuela et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Serotonin-specific neurons differentiated from human iPSCs form distinct subtypes with synaptic protein assembly

(2021) Charline Jansch et al.   JOURNAL OF NEURAL TRANSMISSION

[18F]F13640, a 5-HT1A Receptor Radiopharmaceutical Sensitive to Brain Serotonin Fluctuations

(2021) Matthieu Colom et al.   Frontiers in Neuroscience

Identification of the 5-HT1A serotonin receptor as a novel therapeutic target in a C. elegans model of Machado-Joseph disease

(2021) Joana Pereira-Sousa et al.   NEUROBIOLOGY OF DISEASE

The selective 5-HT1A receptor biased agonists, F15599 and F13714, show antidepressant-like properties after a single administration in the mouse model of unpredictable chronic mild stress

(2021) Monika Głuch-Lutwin et al.   PSYCHOPHARMACOLOGY

Different Alterations of Agonist and Antagonist Binding to 5-HT1A Receptor in a Rat Model of Parkinson’s Disease and Levodopa-Induced Dyskinesia: A microPET Study

(2021) Benjamin Vidal et al.   Journal of Parkinsons Disease

NLX-101, a cortical 5-HT1A receptor biased agonist, reverses scopolamine-induced deficit in the delayed non-matching to position model of cognition

(2021) Ronan Yves Depoortere et al.   BRAIN RESEARCH

Perspectives for therapy of treatment‐resistant depression

(2021) Mariusz Papp et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biased agonism at adenosine receptors

(2021) Samantha M. McNeill et al.   CELLULAR SIGNALLING

Biased agonism in drug discovery: Is there a future for biased 5-HT1A receptor agonists in the treatment of neuropsychiatric diseases?

(2021) Kinga Sałaciak et al.   PHARMACOLOGY & THERAPEUTICS

The selective 5-HT1A receptor agonist, NLX-112, exerts anti-dyskinetic and anti-parkinsonian-like effects in MPTP-treated marmosets

(2020) Ria Fisher et al.   NEUROPHARMACOLOGY

Pharmacological Studies on the Role of 5-HT1A Receptors in Male Sexual Behavior of Wildtype and Serotonin Transporter Knockout Rats

(2020) Diana Carolina Esquivel-Franco et al.   Frontiers in Behavioral Neuroscience

Intrinsic efficacy of opioid ligands and its importance for apparent bias, operational analysis and therapeutic window

(2020) Alexander Gillis et al.   MOLECULAR PHARMACOLOGY

Central 5-HT receptors and their function; present and future

(2020) Trevor Sharp et al.   NEUROPHARMACOLOGY

The selective 5-HT1A receptor agonist, NLX-112, exerts anti-dyskinetic effects in MPTP-treated macaques

(2020) R. Depoortere et al.   PARKINSONISM & RELATED DISORDERS

Interactions Between the Serotonergic and Other Neurotransmitter Systems in the Basal Ganglia: Role in Parkinson’s Disease and Adverse Effects of L-DOPA

(2020) Ana Muñoz et al.   Frontiers in Neuroanatomy

Improvement of lower urinary tract function by a selective serotonin 5-HT1A receptor agonist, NLX-112, after chronic spinal cord injury

(2020) Ching-Yi Lin et al.   EXPERIMENTAL NEUROLOGY

Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT1A Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile

(2020) Joanna Sniecikowska et al.   JOURNAL OF MEDICINAL CHEMISTRY

International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function

(2020) Nicholas M. Barnes et al.   PHARMACOLOGICAL REVIEWS

Innovative approaches in CNS drug discovery

(2020) Mathieu Charvériat et al.   THERAPIE

NLX-101, a highly selective 5-HT1A receptor biased agonist, mediates antidepressant-like activity in rats via prefrontal cortex 5-HT1A receptors

(2020) R. Depoortère et al.   BEHAVIOURAL BRAIN RESEARCH

Biased agonism at chemokine receptors

(2020) Dylan Scott Eiger et al.   CELLULAR SIGNALLING

Biased agonism at the cannabinoid receptors – Evidence from synthetic cannabinoid receptor agonists

(2020) Monica Patel et al.   CELLULAR SIGNALLING

Signaling diversity of mu- and delta- opioid receptor ligands: Re-evaluating the benefits of β-arrestin/G protein signaling bias

(2020) Graciela Pineyro et al.   CELLULAR SIGNALLING

The 5-HT1A receptor as a serotonergic target for neuroprotection in cerebral ischemia

(2020) Rafael Pazinatto de Aguiar et al.   PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

Regulation of dopamine neurotransmission from serotonergic neurons by ectopic expression of the dopamine D2 autoreceptor blocks levodopa-induced dyskinesia

(2019) Rhyomi C. Sellnow et al.   Acta Neuropathologica Communications

Defining Structure–Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D1 Receptor Agonists

(2019) Michael L. Martini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Aryloxyethyl Derivatives of 1-(1-Benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) Phosphorylation-Preferring Serotonin 5-HT1A Receptor-Biased Agonists with Robust Antidepressant-like Activity

(2019) Joanna Sniecikowska et al.   JOURNAL OF MEDICINAL CHEMISTRY

Serotonin 5-HT1A Receptor Biased Agonists Display Differential Anxiolytic Activity in a Rat Social Interaction Model

(2019) Ronan Depoortère et al.   ACS Chemical Neuroscience

Genetic, epigenetic and posttranscriptional mechanisms for treatment of major depression: the 5-HT1A receptor gene as a paradigm

(2019) Paul R. Albert et al.   JOURNAL OF PSYCHIATRY & NEUROSCIENCE

Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential

(2019) Mohammad Seyedabadi et al.   PHARMACOLOGY & THERAPEUTICS

Overcoming Resistance to Selective Serotonin Reuptake Inhibitors: Targeting Serotonin, Serotonin-1A Receptors and Adult Neuroplasticity

(2019) Faranak Vahid-Ansari et al.   Frontiers in Neuroscience

Cortical 5-hydroxytryptamine 1A receptor biased agonist, NLX-101, displays rapid-acting antidepressant-like properties in the rat chronic mild stress model

(2019) Ronan Depoortère et al.   JOURNAL OF PSYCHOPHARMACOLOGY

Enhanced aggressive phenotype of Tph2 knockout rats is associated with diminished 5-HT1A receptor sensitivity

(2019) Deborah G.A. Peeters et al.   NEUROPHARMACOLOGY

Ketamine ameliorates severe traumatic event-induced antidepressant-resistant depression in a rat model through ERK activation

(2019) Chi-Wei Lee et al.   PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

From Receptor Selectivity to Functional Selectivity: The Rise of Biased Agonism in 5-HT1A Receptor Drug Discovery

(2019) Joanna Sniecikowska et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

18F-F13640 PET imaging of functional receptors in humans

(2019) Matthieu Colom et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development

(2019) Stuart P. McCluskey et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Bell-shaped agonist activation of 5-HT1A receptor-coupled Gαi3 G-proteins: Receptor density-dependent switch in receptor signaling

(2019) A. Newman-Tancredi et al.   CELLULAR SIGNALLING

Pharmacological MRI to investigate the functional selectivity of 5-HT1A receptor biased agonists

(2019) Benjamin Vidal et al.   NEUROPHARMACOLOGY

Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?

(2019) Matthieu Colom et al.   Frontiers in Molecular Neuroscience

Activation of 5-HT1A postsynaptic receptors by NLX-101 results in functional recovery and an increase in neuroplasticity in mice with brain ischemia

(2019) Rafael Pazinatto Aguiar et al.   PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

NLX-112, a highly selective 5-HT 1A receptor agonist, mediates analgesia and antidepressant-like activity in rats via spinal cord and prefrontal cortex 5-HT 1A receptors, respectively

(2018) A. Newman-Tancredi et al.   BRAIN RESEARCH

18F-F13640 preclinical evaluation in rodent, cat and primate as a 5-HT1A receptor agonist for PET neuroimaging

(2018) Benjamin Vidal et al.   Brain Structure & Function

Neurophysiological effects in cortico-basal ganglia-thalamic circuits of antidyskinetic treatment with 5-HT 1A receptor biased agonists

(2018) Ivani Brys et al.   EXPERIMENTAL NEUROLOGY

Serotonergic targets for the treatment of l-DOPA-induced dyskinesia

(2018) Kathryn Lanza et al.   JOURNAL OF NEURAL TRANSMISSION

Receptor–Receptor Interactions in Multiple 5-HT1A Heteroreceptor Complexes in Raphe-Hippocampal 5-HT Transmission and Their Relevance for Depression and Its Treatment

(2018) Dasiel Borroto-Escuela et al.   MOLECULES

Effects of the Serotonin 5-HT1A Receptor Biased Agonists, F13714 and F15599, on Striatal Neurotransmitter Levels Following l-DOPA Administration in Hemi-Parkinsonian Rats

(2018) Adrian Newman-Tancredi et al.   NEUROCHEMICAL RESEARCH

5-HT 1A receptor stimulation in the medial prefrontal cortex mediates the antidepressant effects of mGlu2/3 receptor antagonist in mice

(2018) Kenichi Fukumoto et al.   NEUROPHARMACOLOGY

In vivo biased agonism at 5-HT1A receptors: characterisation by simultaneous PET/MR imaging

(2018) Benjamin Vidal et al.   NEUROPSYCHOPHARMACOLOGY

NLX-112, a highly selective 5-HT 1A receptor agonist: Effects on body temperature and plasma corticosterone levels in rats

(2018) A. Newman-Tancredi et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Rapid antidepressant effects of deep brain stimulation of the pre-frontal cortex in an animal model of treatment-resistant depression

(2018) Mariusz Papp et al.   JOURNAL OF PSYCHOPHARMACOLOGY

Serotonin 5-HT1A Receptor Biased Agonists Induce Different Cerebral Metabolic Responses: A [18F]-Fluorodesoxyglucose Positron Emission Tomography Study in Conscious and Anesthetized Rats

(2018) Elise Levigoureux et al.   ACS Chemical Neuroscience

The 5-HT1A receptor: Signaling to behavior

(2018) Paul R. Albert et al.   BIOCHIMIE

Chronic Unpredictable Mild Stress for Modeling Depression in Rodents:Meta-analysis of Model Reliability

(2018) Svitlana Antoniuk et al.   NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS

Activation of somatodendritic 5-HT1A autoreceptors reduces the acquisition and expression of cued fear in the rat fear-potentiated startle test

(2018) Yulong Zhao et al.   PSYCHOPHARMACOLOGY

HBK-17, a 5-HT1A Receptor Ligand With Anxiolytic-Like Activity, Preferentially Activates ß-Arrestin Signaling

(2018) Karolina Pytka et al.   Frontiers in Pharmacology

Characterizing the differential roles of striatal 5-HT 1A auto- and hetero-receptors in the reduction of l -DOPA-induced dyskinesia

(2017) Samantha M. Meadows et al.   EXPERIMENTAL NEUROLOGY

Role of 5-HT1A Receptor Stimulation in the Medial Prefrontal Cortex in the Sustained Antidepressant Effects of Ketamine

(2017) Kenichi Fukumoto et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

The Use of Microdosing in the Development of Small Organic and Protein Therapeutics

(2017) Mats Bergstrom   JOURNAL OF NUCLEAR MEDICINE

Distinctive in vitro signal transduction profile of NLX-112, a potent and efficacious serotonin 5-HT1A receptor agonist

(2017) Adrian Newman-Tancredi et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs

(2017) John D McCorvy et al.   Nature Chemical Biology

Hippocampal 5-HT 1A receptor expression changes in prodromal stages of Alzheimer's disease: Beneficial or deleterious?

(2017) Mathieu Verdurand et al.   NEUROPHARMACOLOGY

Antinociceptive, antiallodynic and antihyperalgesic effects of the 5-HT 1A receptor selective agonist, NLX-112 in mouse models of pain

(2017) Kinga Sałat et al.   NEUROPHARMACOLOGY

Involvement of extracellular signal-regulated kinase (ERK) in the short and long-lasting antidepressant-like activity of NMDA receptor antagonists (zinc and Ro 25-6981) in the forced swim test in rats

(2017) Bartłomiej Pochwat et al.   NEUROPHARMACOLOGY

Response characteristics of the rat anterior cingulate cortex to ultrasonic communicative vocalizations

(2017) Yumi Saito et al.   NEUROREPORT

Involvement of presynaptic 5-HT 1A receptors in the low propensity of brexpiprazole to induce extrapyramidal side effects in rats

(2017) Cedric Mombereau et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Contribution of Clinical Neuroimaging to the Understanding of the Pharmacology of Methylphenidate

(2017) Luc Zimmer   TRENDS IN PHARMACOLOGICAL SCIENCES

Understanding the Role of GPCR Heteroreceptor Complexes in Modulating the Brain Networks in Health and Disease

(2017) Dasiel O. Borroto-Escuela et al.   Frontiers in Cellular Neuroscience

5-hydroxytryptamine 1A (5-HT 1A ) receptor agonists: A decade of empirical evidence supports their use as an efficacious therapeutic strategy for brain trauma

(2016) Jeffrey P. Cheng et al.   BRAIN RESEARCH

Emerging treatment mechanisms for depression: focus on glutamate and synaptic plasticity

(2016) Danielle M. Gerhard et al.   DRUG DISCOVERY TODAY

P.2.015 Chronic effects of ‘biased’ 5-HT1A receptor agonists on object pattern separation performance and hippocampal plasticity

(2016) B. Van Hagen et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

The 5-HT1A receptor in Major Depressive Disorder

(2016) Joshua Kaufman et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Marmoset Serotonin 5-HT1AReceptor Mapping with a Biased Agonist PET Probe18F-F13714: Comparison with an Antagonist Tracer18F-MPPF in Awake and Anesthetized States

(2016) Chihiro Yokoyama et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Systems-level neurophysiological state characteristics for drug evaluation in an animal model of levodopa-induced dyskinesia

(2016) Martin Tamtè et al.   JOURNAL OF NEUROPHYSIOLOGY

Differential effects of amyloid-beta 1–40 and 1–42 fibrils on 5-HT 1A serotonin receptors in rat brain

(2016) Mathieu Verdurand et al.   NEUROBIOLOGY OF AGING

Agonist and antagonist bind differently to 5-HT 1A receptors during Alzheimer’s disease: A post-mortem study with PET radiopharmaceuticals

(2016) Benjamin Vidal et al.   NEUROPHARMACOLOGY

The novel 5-HT 1A receptor agonist, NLX-112 reduces l -DOPA-induced abnormal involuntary movements in rat: A chronic administration study with microdialysis measurements

(2016) Andrew C. McCreary et al.   NEUROPHARMACOLOGY

Pharmacological agonists for more-targeted CNS radio-pharmaceuticals

(2016) Luc Zimmer   Oncotarget

Selective serotonin 5-HT1A receptor biased agonists elicitdistinct brain activation patterns: a pharmacoMRI study

(2016) G. Becker et al.   Scientific Reports

5-HT1A Receptor Agonist Befiradol Reduces Fentanyl-induced Respiratory Depression, Analgesia, and Sedation in Rats

(2015) Jun Ren et al.   ANESTHESIOLOGY

Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2

(2015) Nikolas Stroth et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Eltoprazine counteracts l-DOPA-induced dyskinesias in Parkinson’s disease: a dose-finding study

(2015) Per Svenningsson et al.   BRAIN

Divergent effects of the ‘biased’ 5-HT1Areceptor agonists F15599 and F13714 in a novel object pattern separation task

(2015) N P van Goethem et al.   BRITISH JOURNAL OF PHARMACOLOGY

Serotonin 5-HT1A Receptors and Antipsychotics - An Update in Light of New Concepts and Drugs

(2015) Andrew McCreary et al.   CURRENT PHARMACEUTICAL DESIGN

NLX-112, a novel 5-HT 1A receptor agonist for the treatment of l -DOPA-induced dyskinesia: Behavioral and neurochemical profile in rat

(2015) H. Iderberg et al.   EXPERIMENTAL NEUROLOGY

Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands

(2015) Zdzisław Chilmonczyk et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Activity of serotonin 5-HT1A receptor ‘biased agonists’ in rat models of Parkinson's disease and l-DOPA-induced dyskinesia

(2015) H. Iderberg et al.   NEUROPHARMACOLOGY

The highly-selective 5-HT1A agonist F15599 reduces l-DOPA-induced dyskinesia without compromising anti-parkinsonian benefits in the MPTP-lesioned macaque

(2015) Philippe Huot et al.   NEUROPHARMACOLOGY

Anti-aggressive effects of the selective high-efficacy ‘biased’ 5-HT1A receptor agonists F15599 and F13714 in male WTG rats

(2015) Sietse F. de Boer et al.   PSYCHOPHARMACOLOGY

Optimising PET approaches to measuring 5-HT release in human brain

(2015) Robin J. Tyacke et al.   SYNAPSE

Effect of Sarizotan, a 5-HT1aand D2-Like Receptor Agonist, on Respiration in Three Mouse Models of Rett Syndrome

(2014) Ana P. Abdala et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Side effect profile of 5-HT treatments for Parkinson's disease and L-DOPA-induced dyskinesia in rats

(2014) D Lindenbach et al.   BRITISH JOURNAL OF PHARMACOLOGY

A Postmortem Study to Compare Agonist and Antagonist 5-HT1AReceptor-binding Sites in Alzheimer's Disease

(2014) Guillaume Becker et al.   CNS Neuroscience & Therapeutics

Serotonin-prefrontal cortical circuitry in anxiety and depression phenotypes: pivotal role of pre- and post-synaptic 5-HT1A receptor expression

(2014) Paul R. Albert et al.   Frontiers in Behavioral Neuroscience

Serotonin 5-HT1A Receptors as Targets for Agents to Treat Psychiatric Disorders: Rationale and Current Status of Research

(2013) Pau Celada et al.   CNS DRUGS

PET Radiotracers for Molecular Imaging of Serotonin 5-HT1A Receptors

(2013) T. Billard et al.   CURRENT MEDICINAL CHEMISTRY

A selective 5-HT1a receptor agonist improves respiration in a mouse model of Rett syndrome

(2013) Erica S. Levitt et al.   JOURNAL OF APPLIED PHYSIOLOGY

Development of brainstem 5-HT1Areceptor-binding sites in serotonin-deficient mice

(2013) Caitlin A. Massey et al.   JOURNAL OF NEUROCHEMISTRY

Aggression-reducing effects of F15599, a novel selective 5-HT1A receptor agonist, after microinjection into the ventral orbital prefrontal cortex, but not in infralimbic cortex in male mice

(2013) Dirson João Stein et al.   PSYCHOPHARMACOLOGY

Serotonergic mechanisms are necessary for central respiratory chemoresponsiveness in situ

(2013) Andrea E. Corcoran et al.   RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY

Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

(2013) Enza Lacivita et al.   EXPERIMENTAL BRAIN RESEARCH

Buspirone: What is it all about?

(2012) C. Loane et al.   BRAIN RESEARCH

μ-opioid and 5-HT1A receptors heterodimerize and show signalling crosstalk via G protein and MAP-kinase pathways

(2012) Didier Cussac et al.   CELLULAR SIGNALLING

Radiosynthesis and Preclinical Evaluation of 18F-F13714 as a Fluorinated 5-HT1A Receptor Agonist Radioligand for PET Neuroimaging

(2012) L. Lemoine et al.   JOURNAL OF NUCLEAR MEDICINE

Impaired Chemosensitivity of Mouse Dorsal Raphe Serotonergic Neurons Overexpressing Serotonin 1A (Htr1a) Receptors

(2012) Gilda Baccini et al.   PLoS One

The role of 5-HT1A receptors in phencyclidine (PCP)-induced novel object recognition (NOR) deficit in rats

(2012) M. Horiguchi et al.   PSYCHOPHARMACOLOGY

Biased agonism at serotonin 5-HT1A receptors: preferential postsynaptic activity for improved therapy of CNS disorders

(2012) Adrian Newman-Tancredi   Neuropsychiatry

Role of 5-HT1 receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn

(2011) Hyo-Jin Jeong et al.   BRITISH JOURNAL OF PHARMACOLOGY

5-HT1A Receptor Agonists Enhance Pyramidal Cell Firing in Prefrontal Cortex Through a Preferential Action on GABA Interneurons

(2011) L. Llado-Pelfort et al.   CEREBRAL CORTEX

Continuous drug delivery in early- and late-stage Parkinson’s disease as a strategy for avoiding dyskinesia induction and expression

(2011) P. Jenner et al.   JOURNAL OF NEURAL TRANSMISSION

Serotonin-1A receptors in major depression quantified using PET: Controversies, confounds, and recommendations

(2011) Saurav Shrestha et al.   NEUROIMAGE

In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat

(2011) Laia Lladó-Pelfort et al.   PSYCHOPHARMACOLOGY

Preferential in vivo action of F15599, a novel 5-HT1A receptor agonist, at postsynaptic 5-HT1A receptors

(2010) L Lladó-Pelfort et al.   BRITISH JOURNAL OF PHARMACOLOGY

5-HT1A receptor-regulated signal transduction pathways in brain

(2010) Abigail M. Polter et al.   CELLULAR SIGNALLING

Competitive interaction of 5-HT1A receptors with G-protein subtypes in CHO cells demonstrated by RNA interference

(2010) Isabelle Rauly-Lestienne et al.   CELLULAR SIGNALLING

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

(2010) Nagarajan Vaidehi et al.   CURRENT OPINION IN PHARMACOLOGY

F15599, a preferential post-synaptic 5-HT1A receptor agonist: Activity in models of cognition in comparison with reference 5-HT1A receptor agonists

(2010) Ronan Depoortère et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

F15599, a highly selective post-synaptic 5-HT1A receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity

(2010) Marie-Bernadette Assié et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Measuring Endogenous 5-HT Release by Emission Tomography: Promises and Pitfalls

(2010) Louise M Paterson et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Novel Pyridylmethylamines as Highly Selective 5-HT1ASuperagonists

(2010) Stefan Bollinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multifunctional Pharmacology of Flibanserin: Possible Mechanism of Therapeutic Action in Hypoactive Sexual Desire Disorder

(2010) Stephen M. Stahl et al.   Journal of Sexual Medicine

The Serotonin Transporter Plays an Important Role in Male Sexual Behavior: A Study in Serotonin Transporter Knockout Rats

(2010) Johnny S.W. Chan et al.   Journal of Sexual Medicine

[3H]-F13640, a novel, selective and high-efficacy serotonin 5-HT1A receptor agonist radioligand

(2010) Peter Heusler et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: A PET study in a receptor internalization-deficient mouse model

(2010) Mette Skinbjerg et al.   NEUROIMAGE

Correction of respiratory disorders in a mouse model of Rett syndrome

(2010) A. P. L. Abdala et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice

(2009) Liesbeth A. Bruins Slot et al.   BEHAVIOURAL PHARMACOLOGY

Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1Areceptor agonist

(2009) A Newman-Tancredi et al.   BRITISH JOURNAL OF PHARMACOLOGY

[18F]F15599, a novel 5-HT1A receptor agonist, as a radioligand for PET neuroimaging

(2009) Laëtitia Lemoine et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Food restriction and streptozotocin differentially modify sensitivity to the hypothermic effects of direct- and indirect-acting serotonin receptor agonists in rats

(2009) Jun-Xu Li et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Triptans, Serotonin Agonists, and Serotonin Syndrome (Serotonin Toxicity): A Review

(2009) P. Ken Gillman   HEADACHE

Agonist-dependent modulation of G-protein coupling and transduction of 5-HT1A receptors in rat dorsal raphe nucleus

(2009) Elsa Maria Valdizán et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Aberrant extracellular signal-regulated kinase (ERK)1/2 signalling in suicide brain: role of ERK kinase 1 (MEK1)

(2009) Yogesh Dwivedi et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Cellular assays as portals to seven-transmembrane receptor-based drug discovery

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

Effects of amyloid-β peptides on the serotoninergic 5-HT1A receptors in the rat hippocampus

(2009) Mathieu Verdurand et al.   NEUROBIOLOGY OF AGING

5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice

(2009) Alex Brenchat et al.   PAIN

Loss of MeCP2 in aminergic neurons causes cell-autonomous defects in neurotransmitter synthesis and specific behavioral abnormalities

(2009) R. C. Samaco et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Breathing disorders in Rett syndrome: Progressive neurochemical dysfunction in the respiratory network after birth

(2009) David M. Katz et al.   RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY

The role of 5-HT1A receptors in learning and memory

(2008) Sven Ove Ögren et al.   BEHAVIOURAL BRAIN RESEARCH

Does stimulation of 5-HT1A receptors improve cognition in schizophrenia?

(2008) Herbert Y. Meltzer et al.   BEHAVIOURAL BRAIN RESEARCH

Combined 5-HT1A and 5-HT1B receptor agonists for the treatment of L-DOPA-induced dyskinesia

(2008) A. Munoz et al.   BRAIN

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells

(2008) Didier Cussac et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Assessing human 5-HT function in vivo with pharmacoMRI

(2008) I.M. Anderson et al.   NEUROPHARMACOLOGY

Region-specific changes in 5-HT1A agonist-induced Extracellular signal-Regulated Kinases 1/2 phosphorylation in rat brain: A quantitative ELISA study

(2008) Jaroslava Buritova et al.   NEUROPHARMACOLOGY

Unfaithful neurotransmitter transporters: Focus on serotonin uptake and implications for antidepressant efficacy

(2008) Lynette C. Daws   PHARMACOLOGY & THERAPEUTICS

Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions

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

Rapid desensitization of somatodendritic 5-HT1A receptors by chronic administration of the high-efficacy 5-HT1A agonist, F13714: a microdialysis study in the rat

(2006) M-B Assié et al.   BRITISH JOURNAL OF PHARMACOLOGY