Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants

W Duan, D Cao, S Wang, J Cheng - Chemical Reviews, 2023 - ACS Publications
Psychedelics make up a group of psychoactive compounds that induce hallucinogenic
effects by activating the serotonin 2A receptor (5-HT2AR). Clinical trials have demonstrated …

New therapeutic opportunities for 5-HT2C receptor ligands in neuropsychiatric disorders

G Di Giovanni, P De Deurwaerdère - Pharmacology & therapeutics, 2016 - Elsevier
Abstract The 5-HT 2C receptor (R) displays a widespread distribution in the CNS and is
involved in the action of 5-HT in all brain areas. Knowledge of its functional role in the CNS …

Synthesis of monofluoroalkenes: a leap forward

M Drouin, JD Hamel, JF Paquin - Synthesis, 2018 - thieme-connect.com
Monofluoroalkenes have found wide application in organic chemistry, medicinal chemistry,
and materials science. This review summarizes the most recent advances made regarding …

Lorcaserin: A review of its preclinical and clinical pharmacology and therapeutic potential

GA Higgins, PJ Fletcher, WR Shanahan - Pharmacology & Therapeutics, 2020 - Elsevier
The selective 5-HT2C receptor agonist lorcaserin, in conjunction with lifestyle modification,
was approved by the FDA in 2012 for weight management. It has been marketed in the US …

Palladium-Catalyzed Ring-Opening Coupling of gem-Difluorocyclopropanes for the Construction of 2-Fluoroallylic Sulfones

J Ni, B Nishonov, A Pardaev… - The Journal of Organic …, 2019 - ACS Publications
A Pd-catalyzed ring-opening sulfonylation of gem-difluorocyclopropanes is reported. This
protocol involves C–C bond cleavage, β-F elimination, and allylic coupling to form …

Design and synthesis of novel gpr139 agonists with therapeutic effects in mouse models of social interaction and cognitive impairment

J Mao, Y Cui, H Wang, W Duan, ZJ Liu… - Journal of Medicinal …, 2023 - ACS Publications
The GPR139 receptor is an orphan G-protein-coupled receptor (GPCR) mainly found in the
central nervous system and is a potential therapeutic target for the treatment of …

Targeting the 5-HT2C receptor in biological context and the current state of 5-HT2C receptor ligand development

EA Wold, CT Wild, KA Cunningham… - Current topics in …, 2019 - ingentaconnect.com
Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of
diseaserelated pathways and behaviors based upon actions in the central nervous system …

Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis

Y Wang, W Lin, N Wu, S Wang, M Chen, Z Lin… - Acta Pharmacologica …, 2019 - nature.com
Abstract Serotonin (5-HT) receptors are proteins involved in various neurological and
biological processes, such as aggression, anxiety, appetite, cognition, learning, memory …

5-HT2C agonists modulate schizophrenia-like behaviors in mice

VM Pogorelov, RM Rodriguiz, J Cheng… - …, 2017 - nature.com
All FDA-approved antipsychotic drugs (APDs) target primarily dopamine D 2 or serotonin (5-
HT 2A) receptors, or both; however, these medications are not universally effective, they may …

The impact of the secondary binding pocket on the pharmacology of class A GPCRs

A Egyed, DJ Kiss, GM Keserű - Frontiers in pharmacology, 2022 - frontiersin.org
G-protein coupled receptors (GPCRs) are considered important therapeutic targets due to
their pathophysiological significance and pharmacological relevance. Class A receptors …