In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor 5‐HT 2A R

Synthesis and Functional Characterization of 2-(2,5-Dimethoxyphenyl)-N-(2-fluorobenzyl)ethanamine (25H-NBF) Positional Isomers

(2021) Eline Pottie et al.   ACS Chemical Neuroscience

Trial of Psilocybin versus Escitalopram for Depression

(2021) Robin Carhart-Harris et al.   NEW ENGLAND JOURNAL OF MEDICINE

Psychedelics and Other Psychoplastogens for Treating Mental Illness

(2021) Maxemiliano V. Vargas et al.   Frontiers in Psychiatry

Investigation of the 2,5-Dimethoxy Motif in Phenethylamine Serotonin 2A Receptor Agonists

(2020) Emil Marcher-Rørsted et al.   ACS Chemical Neuroscience

Designer drugs: mechanism of action and adverse effects

(2020) Dino Luethi et al.   ARCHIVES OF TOXICOLOGY

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

(2020) Reid H. J. Olsen et al.   Nature Chemical Biology

In vitro structure–activity relationship determination of 30 psychedelic new psychoactive substances by means of β-arrestin 2 recruitment to the serotonin 2A receptor

(2020) Eline Pottie et al.   ARCHIVES OF TOXICOLOGY

Differential signaling signatures evoked by DOI versus lisuride stimulation of the 5-HT2A receptor

(2020) Antara A. Banerjee et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

In vitro characterization of new psychoactive substances at the µ-opioid, CB1, 5HT1A, and 5-HT2A receptors—On-target receptor potency and efficacy, and off-target effects

(2020) Anna Åstrand et al.   FORENSIC SCIENCE INTERNATIONAL

Therapeutic effects of classic serotonergic psychedelics: A systematic review of modern‐era clinical studies

(2020) Kristoffer A. A. Andersen et al.   ACTA PSYCHIATRICA SCANDINAVICA

Identification of psychedelic new psychoactive substances (NPS) showing biased agonism at the 5-HT2AR through simultaneous use of β-arrestin 2 and miniGαq bioassays

(2020) Eline Pottie et al.   BIOCHEMICAL PHARMACOLOGY

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

Biased Receptor Signaling in Drug Discovery

(2019) Terry Kenakin   PHARMACOLOGICAL REVIEWS

Monoamine receptor interaction profiles of 4-aryl-substituted 2,5-dimethoxyphenethylamines (2C-BI derivatives)

(2019) Dino Luethi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Setup of a Serotonin 2A Receptor (5-HT2AR) Bioassay: Demonstration of Its Applicability To Functionally Characterize Hallucinogenic New Psychoactive Substances and an Explanation Why 5-HT2AR Bioassays Are Not Suited for Universal Activity-Based Screening of Biofluids for New Psychoactive Substances

(2019) Eline Pottie et al.   ANALYTICAL CHEMISTRY

Insights into biased signaling at cannabinoid receptors: synthetic cannabinoid receptor agonists

(2019) Elise Wouters et al.   BIOCHEMICAL PHARMACOLOGY

Pharmacological and biotransformation studies of 1-acyl-substituted derivatives of -lysergic acid diethylamide (LSD)

(2019) Adam L. Halberstadt et al.   NEUROPHARMACOLOGY

Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines

(2019) Karolina E. Kolaczynska et al.   Frontiers in Pharmacology

Serotonin 5-HT2A receptor expression and functionality in postmortem frontal cortex of subjects with schizophrenia: Selective biased agonism via Gαi1-proteins

(2019) Aintzane García-Bea et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Monoamine Transporter and Receptor Interaction Profiles in Vitro Predict Reported Human Doses of Novel Psychoactive Stimulants and Psychedelics

(2018) Dino Luethi et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

(2018) Qingwen Wan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Comparative neuropharmacology of N -(2-methoxybenzyl)-2,5-dimethoxyphenethylamine (NBOMe) hallucinogens and their 2C counterparts in male rats

(2018) Joshua S. Elmore et al.   NEUROPHARMACOLOGY

Monoamine receptor interaction profiles of 4-thio-substituted phenethylamines (2C-T drugs)

(2018) Dino Luethi et al.   NEUROPHARMACOLOGY

Ultrafast neuronal imaging of dopamine dynamics with designed genetically encoded sensors

(2018) Tommaso Patriarchi et al.   SCIENCE

Neurochemical pharmacology of psychoactive substituted N-benzylphenethylamines: high potency agonists at 5-HT2A receptors

(2018) Amy J Eshleman et al.   BIOCHEMICAL PHARMACOLOGY

Pharmacological characterization of the LSD analog N-ethyl-N-cyclopropyl lysergamide (ECPLA)

(2018) Adam L. Halberstadt et al.   PSYCHOPHARMACOLOGY

Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N -(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT 2A Receptor Agonist

(2017) Anders A. Jensen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A kinetic view of GPCR allostery and biased agonism

(2017) J Robert Lane et al.   Nature Chemical Biology

The Therapeutic Potential of Psychedelic Drugs: Past, Present, and Future

(2017) Robin L Carhart-Harris et al.   NEUROPSYCHOPHARMACOLOGY

The Diverse Roles of Arrestin Scaffolds in G Protein–Coupled Receptor Signaling

(2017) Yuri K. Peterson et al.   PHARMACOLOGICAL REVIEWS

New therapeutic opportunities for 5-HT2 receptor ligands

(2017) Luc Maroteaux et al.   PHARMACOLOGY & THERAPEUTICS

Mini-G proteins: Novel tools for studying GPCRs in their active conformation

(2017) Rony Nehmé et al.   PLoS One

Systematic errors in detecting biased agonism: Analysis of current methods and development of a new model-free approach

(2017) H. Ongun Onaran et al.   Scientific Reports

5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism

(2016) Sebastian Leth-Petersen et al.   ACS Chemical Neuroscience

IP3 accumulation and/or inositol depletion: two downstream lithium’s effects that may mediate its behavioral and cellular changes

(2016) Y Sade et al.   Translational Psychiatry

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

(2015) Andrew S. Dixon et al.   ACS Chemical Biology

N-Benzyl-5-methoxytryptamines as Potent Serotonin 5-HT2 Receptor Family Agonists and Comparison with a Series of Phenethylamine Analogues

(2015) David E. Nichols et al.   ACS Chemical Neuroscience

Recent advances in the neuropsychopharmacology of serotonergic hallucinogens

(2015) Adam L. Halberstadt   BEHAVIOURAL BRAIN RESEARCH

Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists

(2015) Martin Hansen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Gaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessors

(2015) Terry Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacological profile of novel psychoactive benzofurans

(2015) Anna Rickli et al.   BRITISH JOURNAL OF PHARMACOLOGY

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Receptor interaction profiles of novel N-2-methoxybenzyl (NBOMe) derivatives of 2,5-dimethoxy-substituted phenethylamines (2C drugs)

(2015) Anna Rickli et al.   NEUROPHARMACOLOGY

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Synthesis and Structure–Activity Relationships of N-Benzyl Phenethylamines as 5-HT2A/2C Agonists

(2014) Martin Hansen et al.   ACS Chemical Neuroscience

G Protein-Coupled Receptor Signaling Analysis Using Homogenous Time-Resolved Förster Resonance Energy Transfer (HTRF®) Technology

(2014) Lenea Nørskov-Lauritsen et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Quantitative Phosphoproteomics Unravels Biased Phosphorylation of Serotonin 2A Receptor at Ser280by HallucinogenicversusNonhallucinogenic Agonists

(2014) Samah Karaki et al.   MOLECULAR & CELLULAR PROTEOMICS

Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes

(2014) Bruce E. Blough et al.   PSYCHOPHARMACOLOGY

An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: Emerging ‘Novel Psychoactive Drugs’

(2013) Warunya Arunotayanun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Behavioral and neurochemical pharmacology of six psychoactive substituted phenethylamines: mouse locomotion, rat drug discrimination and in vitro receptor and transporter binding and function

(2013) Amy J. Eshleman et al.   PSYCHOPHARMACOLOGY

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Extensive Rigid Analogue Design Maps the Binding Conformation of Potent N-Benzylphenethylamine 5-HT2A Serotonin Receptor Agonist Ligands

(2012) Jose I. Juncosa et al.   ACS Chemical Neuroscience

Tools for GPCR drug discovery

(2012) Ru Zhang et al.   ACTA PHARMACOLOGICA SINICA

Mammalian Phospholipase C

(2012) Ganesh Kadamur et al.   Annual Review of Physiology

trans-2-(2,5-Dimethoxy-4-iodophenyl)cyclopropylamine andtrans-2-(2,5-dimethoxy-4-bromophenyl)cyclopropylamine as potent agonists for the 5-HT2receptor family

(2012) Adam Pigott et al.   Beilstein Journal of Organic Chemistry

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

5-HT2Areceptor signalling through phospholipase D1 associated with its C-terminal tail

(2011) Zoë Barclay et al.   BIOCHEMICAL JOURNAL

Abuse Liability Profile of Three Substituted Tryptamines

(2011) M. B. Gatch et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

Schizophrenia risk gene CAV1 is both pro-psychotic and required for atypical antipsychotic drug actions in vivo

(2011) J A Allen et al.   Translational Psychiatry

Exploring a role for heteromerization in GPCR signalling specificity

(2010) Raphael Rozenfeld et al.   BIOCHEMICAL JOURNAL

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

(2010) Steven J Charlton et al.   BRITISH JOURNAL OF PHARMACOLOGY

Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers

(2010) Anders Ettrup et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Radiosynthesis and Evaluation of 11C-CIMBI-5 as a 5-HT2A Receptor Agonist Radioligand for PET

(2010) A. Ettrup et al.   JOURNAL OF NUCLEAR MEDICINE

The 5-HT2A serotonin receptor enhances cell viability, affects cell cycle progression and activates MEK–ERK1/2 and JAK2–STAT3 signalling pathways in human choriocarcinoma cell lines

(2010) T. Oufkir et al.   PLACENTA

Psychedelics and the Human Receptorome

(2010) Thomas S. Ray   PLoS One

4-Aryl-Substituted 2,5-Dimethoxyphenethylamines: Synthesis and Serotonin 5-HT2AReceptor Affinities

(2009) Daniel Trachsel et al.   CHEMISTRY & BIODIVERSITY

Differences in the C-terminus contribute to variations in trafficking between rat and human 5-HT2Areceptor isoforms: identification of a primate-specific tripeptide ASK motif that confers GRK-2 and β arrestin-2 interactions

(2009) Aditi Bhattacharya et al.   JOURNAL OF NEUROCHEMISTRY

PSD-95 Is Essential for Hallucinogen and Atypical Antipsychotic Drug Actions at Serotonin Receptors

(2009) A. I. Abbas et al.   JOURNAL OF NEUROSCIENCE

‘Hybrid’ benzofuran–benzopyran congeners as rigid analogs of hallucinogenic phenethylamines

(2008) Danielle M. Schultz et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Serotonin Receptors

(2008) David E. Nichols et al.   CHEMICAL REVIEWS

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

Identification of a serotonin/glutamate receptor complex implicated in psychosis

(2008) Javier González-Maeso et al.   NATURE

Pharmacological properties and discriminative stimulus effects of a novel and selective 5-HT2 receptor agonist AL-38022A [(S)-2-(8,9-dihydro-7H-pyrano[2,3-g]indazol-1-yl)-1-methylethylamine]

(2008) Jesse A. May et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Agonist-directed signaling of the serotonin 2A receptor depends on  -arrestin-2 interactions in vivo

(2008) C. L. Schmid et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

High-Affinity Agonist Binding Correlates with Efficacy (Intrinsic Activity) at the Human Serotonin 5-HT2A and 5-HT2C Receptors: Evidence Favoring the Ternary Complex and Two-State Models of Agonist Action

(2003) Lawrence W. Fitzgerald et al.   JOURNAL OF NEUROCHEMISTRY

Structure and Function of the Third Intracellular Loop of the 5-Hydroxytryptamine2A Receptor: The Third Intracellular Loop Is α-Helical and Binds Purified Arrestins

(2003) Edward I. Gelber et al.   JOURNAL OF NEUROCHEMISTRY