International Union of Basic and Clinical Pharmacology. CX. Classification of receptors for 5-hydroxytryptamine; pharmacology and function

NM Barnes, GP Ahern, C Becamel, J Bockaert… - Pharmacological …, 2021 - ASPET
5-HT receptors expressed throughout the human body are targets for established
therapeutics and various drugs in development. Their diversity of structure and function …

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

B Benhamú, M Martín-Fontecha… - Journal of medicinal …, 2014 - ACS Publications
Alzheimer's disease (AD) is one of the most frequent causes of death and disability
worldwide and has a significant clinical and socioeconomic impact. In the search for novel …

Effect of masupirdine (SUVN‐502) on cognition in patients with moderate Alzheimer's disease: A randomized, double‐blind, phase 2, proof‐of‐concept study

R Nirogi, J Ieni, VK Goyal, J Ravula… - … Research & Clinical …, 2022 - Wiley Online Library
Introduction This study explored the efficacy and safety of a serotonin‐6 receptor antagonist,
masupirdine, as adjunct treatment in patients with moderate Alzheimer's disease (AD) …

Peripheral 5-HT/HTR6 axis is responsible for obesity-associated hypertension

VI Chechekhin, AM Ivanova, KY Kulebyakin… - … et Biophysica Acta (BBA …, 2024 - Elsevier
Hypertension is one of the major life-threatening complications of obesity. Recently adipose
multipotent mesenchymal stromal cells (MSCs) were implicated to the pathogenesis of …

[PDF][PDF] Constitutive activity of serotonin receptor 6 regulates human cerebral organoids formation and depression-like behaviors

Q Wang, X Dong, T Hu, C Qu, J Lu, Y Zhou, J Li, G Pei - Stem Cell Reports, 2021 - cell.com
Summary Serotonin receptor 6 (5-HT 6 R), a typical G protein-coupled receptor (GPCR)
mainly expressed in the neurogenic area with constitutive activity, is of particular interest as …

Syntheses, Radiolabelings, and in Vitro Evaluations of Fluorinated PET Radioligands of 5-HT6 Serotoninergic Receptors

J Colomb, G Becker, S Fieux, L Zimmer… - Journal of Medicinal …, 2014 - ACS Publications
The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases
(schizophrenia, Alzheimer's disease, etc.). However, with lack of specific …

SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization

R Nirogi, R Abraham, V Benade… - Behavioural …, 2019 - journals.lww.com
Research in Alzheimer's disease is going through a big turnaround. New palliative therapies
are being reconsidered for the effective management of disease because of setbacks in the …

Classification and signaling characteristics of 5-HT receptors: toward the concept of 5-HT receptosomes

P Marin, C Becamel, S Chaumont-Dubel… - Handbook of behavioral …, 2020 - Elsevier
Abstract Serotonin (5-hydroxytryptamine, 5-HT) is one of the extracellular messengers
capable of activating the largest number of receptors (17 receptors belonging to seven …

The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1, 3, 5-triazine

D Łażewska, R Kurczab, M Więcek, K Kamińska… - European Journal of …, 2017 - Elsevier
The work describes a discovery of new chemical family of potent ligands for the 5-HT 6
serotonin receptors. During the search for new histamine H 4 receptor antagonists among 1 …

Structural insights into constitutive activity of 5-HT6 receptor

L He, Q Zhao, J Qi, Y Wang, W Han… - Proceedings of the …, 2023 - National Acad Sciences
While most therapeutic research on G-protein-coupled receptors (GPCRs) focuses on
receptor activation by (endogenous) agonists, significant therapeutic potential exists through …