4.7 Article

Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT2C Receptor and Dual 5-HT2C/5-HT2A Receptor Modulators

Related references

Note: Only part of the references are listed.
Review Psychiatry

Psychedelics as Transformative Therapeutics

Bryan L. Roth et al.

Summary: In the past decade, psychedelic compounds have gained attention as potential transformative therapeutics for various neuropsychiatric conditions. However, most of the previous research has focused on understanding their interaction with neurotransmitter systems, particularly the serotonin 5-HT2A receptor. With the recent interest in utilizing these compounds as therapeutics and the increase in clinical trials, psychedelics have shown promise in treating neuro-psychiatric disorders such as depression, cluster headaches, migraines, anxiety, and obsessive-compulsive disorder. It is important to understand the biology and pharmacology behind their therapeutic mechanisms and identify any potential pitfalls in their widespread use as treatments. This review covers the latest advances in understanding their biological mechanisms, ongoing efforts in drug discovery, and potential challenges in utilizing these compounds as emerging therapeutics.

AMERICAN JOURNAL OF PSYCHIATRY (2023)

Article Multidisciplinary Sciences

Establishment of multi-stage intravenous self-administration paradigms in mice

Lauren M. M. Slosky et al.

Summary: Genetically tractable animal models provide an important strategy to understand the biological basis of drug addiction. Using IVSA paradigms for mice, researchers were able to model addiction behavior and identify latent variables such as incentive motivation and discriminative control. Machine learning revealed that vulnerability to drug seeking and relapse in mice could be predicted based on their response to novelty and drug-induced locomotion.

SCIENTIFIC REPORTS (2022)

Review Pharmacology & Pharmacy

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

Nicholas M. Barnes et al.

Summary: This review provides a comprehensive account of the classification and function of 5-hydroxytryptamine receptors, including how they are targeted for therapeutic benefit.

PHARMACOLOGICAL REVIEWS (2021)

Review Chemistry, Medicinal

Spotlight on Pimavanserin Tartrate and Its Therapeutic Potential in the Treatment of Major Depressive Disorder: The Evidence to Date

Vicki Soogrim et al.

Summary: Pimavanserin may be a potential adjunctive treatment for MDD, showing significant improvement in specific symptoms, but its availability for clinical care remains uncertain.

DRUG DESIGN DEVELOPMENT AND THERAPY (2021)

Review Psychiatry

Psychedelics and Other Psychoplastogens for Treating Mental Illness

Maxemiliano V. Vargas et al.

Summary: Psychedelics offer new hope for treating brain disorders due to their sustained therapeutic effects and broad potential, but face challenges in clinical scalability. Research on psychoplastogens provides insight into neural plasticity and offers a new paradigm for addressing the underlying pathophysiology of mental illness. Effectively deploying psychoplastogenic medicines at scale will be a key consideration for future development in the field.

FRONTIERS IN PSYCHIATRY (2021)

Review Endocrinology & Metabolism

Role of serotonin in body weight, insulin secretion and glycaemic control

Teodora Georgescu et al.

Summary: This paper discusses the role of serotonin in energy balance and weight regulation, as well as the potential effects of 5-HT2CR agonists in combating obesity and type 2 diabetes.

JOURNAL OF NEUROENDOCRINOLOGY (2021)

Article Chemistry, Physical

OPLS4: Improving Force Field Accuracy on Challenging Regimes of Chemical Space

Chao Lu et al.

Summary: The development and validation of the OPLS4 force field, which builds upon previous work with OPLS3e, improved model accuracy on challenging regimes of drug-like chemical space. A novel parametrization strategy for charged species was introduced, leading to improved accuracy on benchmarks assessing small-molecule solvation and protein-ligand binding.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2021)

Review Chemistry, Medicinal

hERG toxicity assessment: Useful guidelines for drug design

Amanda Garrido et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Biochemistry & Molecular Biology

Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

Kuglae Kim et al.

Article Biochemistry & Molecular Biology

In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5-HT2 and α1 receptors

Hui Li Heng et al.

CHEMICAL BIOLOGY & DRUG DESIGN (2019)

Article Chemistry, Medicinal

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts

Eric A. Wold et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Chemistry, Medicinal

Targeting the 5-HT2C Receptor in Biological Context and the Current State of 5-HT2C Receptor Ligand Development

Eric A. Wold et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Endogenous Serotonin 5-HT2A and 5-HT2C Receptors Associate in the Medial Prefrontal Cortex

Amanda E. Price et al.

ACS CHEMICAL NEUROSCIENCE (2019)

Article Biochemistry & Molecular Biology

5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology

Yao Peng et al.

Article Biochemistry & Molecular Biology

ProTox-II: a webserver for the prediction of toxicity of chemicals

Priyanka Banerjee et al.

NUCLEIC ACIDS RESEARCH (2018)

Article Multidisciplinary Sciences

Biophysical validation of serotonin 5-HT2A and 5-HT2C receptor interaction

Daniel E. Felsing et al.

PLOS ONE (2018)

Review Chemistry, Medicinal

GPCR Allosteric Modulators: Mechanistic Advantages and Therapeutic Applications

Eric A. Wold et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers

Imane Moutkine et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2017)

Article Chemistry, Medicinal

A Positive Allosteric Modulator of the Serotonin 5-HT2c Receptor for Obesity

Javier Garcia-Carceles et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Biochemistry & Molecular Biology

Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery

Travis T. Wager et al.

ACS CHEMICAL NEUROSCIENCE (2016)

Review Behavioral Sciences

Endocannabinoids and sleep

Oscar Prospero-Garcia et al.

NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS (2016)

Article Clinical Neurology

5-HT2C receptors in psychiatric disorders: A review

A. Chagraoui et al.

PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY (2016)

Article Biochemistry & Molecular Biology

Serotonin (5-HT) 5-HT2A Receptor (5-HT2AR):5-HT2cR Imbalance in Medial Prefrontal Cortex Associates with Motor Impulsivity

Noelle C. Anastasio et al.

ACS CHEMICAL NEUROSCIENCE (2015)

Review Pharmacology & Pharmacy

The role of serotonin 5-HT2A receptors in memory and cognition

Gongliang Zhang et al.

FRONTIERS IN PHARMACOLOGY (2015)

Article Chemistry, Medicinal

Harnessing Allostery: A Novel Approach to Drug Discovery

Shaoyong Lu et al.

MEDICINAL RESEARCH REVIEWS (2014)

Article Multidisciplinary Sciences

Automated design of ligands to polypharmacological profiles

Jeremy Besnard et al.

NATURE (2012)

Article Clinical Neurology

Oleamide administered into the nucleus accumbens shell regulates feeding behaviour via CB1 and 5-HT2C receptors

Edgar Soria-Gomez et al.

INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY (2010)

Article Pharmacology & Pharmacy

Interaction of 5-HT2A and 5-HT2C Receptors in R(-)-2,5-Dimethoxy-4-iodoamphetamine-Elicited Head Twitch Behavior in Mice

W. E. Fantegrossi et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2010)

Review Biotechnology & Applied Microbiology

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

P. Jeffrey Conn et al.

NATURE REVIEWS DRUG DISCOVERY (2009)

Article Neurosciences

5-HT2A and 5-HT2C Receptors Exert Opposing Effects on Locomotor Activity in Mice

Adam L. Halberstadt et al.

NEUROPSYCHOPHARMACOLOGY (2009)

Review Pharmacology & Pharmacy

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

Mark J. Millan et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2008)

Article Behavioral Sciences

Locomotor activity predicts acquisition of self-administration behavior but not cocaine intake

JM Mitchell et al.

BEHAVIORAL NEUROSCIENCE (2005)

Article Pharmacology & Pharmacy

Serotonin 5-HT2A receptors underlie increased motor behaviors induced in dopamine-depleted rats by intrastriatal 5-HT2A/2C agonism

C Bishop et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2004)

Article Pharmacology & Pharmacy

Positive allosteric modulator of the human 5-HT2C receptor

W Bin Im et al.

MOLECULAR PHARMACOLOGY (2003)

Article Multidisciplinary Sciences

No hypothermic response to serotonin in 5-HT7 receptor knockout mice

PB Hedlund et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2003)

Article Behavioral Sciences

Modulation of 5-HT2A receptor-mediated head-twitch behaviour in the rat by 5-HT2C receptor agonists

SP Vickers et al.

PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR (2001)