Drug discovery targeting human 5-HT2C receptors: Residues S3. 36 and Y7. 43 impact ligand—Binding pocket structure via hydrogen bond formation

CE Canal, TC Cordova-Sintjago, NY Villa… - European journal of …, 2011 - Elsevier
Specific activation of serotonin (5-HT) 5-HT2C G protein-coupled receptors may be
therapeutic for obesity and neuropsychiatric disorders. Mutagenesis coupled with …

Agomelatine modulates calcium signaling through protein kinase C and phospholipase C‐mediated mechanisms in rat sensory neurons

I Serhatlioglu, B Bilgin, E Kacar, S Ozcan… - Journal of cellular …, 2019 - Wiley Online Library
Agomelatine, a novel antidepressant exerting its effects through melatonergic and
serotonergic systems, implicated to be effective against pain including neuropathic pain but …

Insights into the influence of 5-HT2c aminoacidic variants with the inhibitory action of serotonin inverse agonists and antagonists

R Galeazzi, L Massaccesi, F Piva, G Principato… - Journal of molecular …, 2014 - Springer
Specific modulation of serotonin 5-HT 2C G protein-coupled receptors may be therapeutic
for obesity and neuropsychiatric disorders. The different efficacy of drugs targeting these …

Cross-species translational findings in the discriminative stimulus effects of ethanol

DC Allen, MM Ford, KA Grant - The Behavioral Neuroscience of Drug …, 2018 - Springer
The progress on understanding the pharmacological basis of ethanol's discriminative
stimulus effects has been substantial, but appears to have plateaued in the past decade …

Aromatic interactions impact ligand binding and function at serotonin 5-HT2C G protein-coupled receptors: receptor homology modelling, ligand docking, and …

T Córdova-Sintjago, N Villa, L Fang, RG Booth - Molecular physics, 2014 - Taylor & Francis
The serotonin (5-hydroxytryptamine, 5-HT) 5-HT2 G protein-coupled receptor (GPCR) family
consists of types 2A, 2B, and 2C that share∼ 75% transmembrane (TM) sequence identity …

Serotonin Receptors of 5-HT2 Type in the Hypothalamic Arcuate Nuclei Positively Regulate Liver Cytochrome P450 via Stimulation of the Growth Hormone–Releasing …

E Bromek, M Rysz, A Haduch, WA Daniel - Drug Metabolism and …, 2019 - ASPET
Our recent study carried out after local injection of the serotonergic neurotoxin 5, 7-
dihydroxytryptamine into the arcuate nucleus (ARC) of the hypothalamus suggested a …

Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT2C Receptors

F Zeng, JA Nye, RJ Voll, L Howell… - ACS Medicinal …, 2018 - ACS Publications
Nine pyridyloxypyridyl indole carboxamides were synthesized and displayed high affinities
for 5-HT2C receptors and high selectivity over 5-HT2A and 5-HT2B. Among them, 6-methyl …

[HTML][HTML] Urocortin1-induced anorexia is regulated by activation of the serotonin 2C receptor in the brain

Y Harada, K Takayama, S Ro, M Ochiai, M Noguchi… - Peptides, 2014 - Elsevier
This study was conducted to determine the mechanisms by which serotonin (5-
hydroxytryptamine, 5-HT) receptors are involved in the suppression of food intake in a rat …

Complex role of the serotonin receptors in depression: Implications for treatment

M Amidfar, L Colic, M Walter, YK Kim - Understanding Depression: Volume …, 2018 - Springer
Evidence from pharmacological, neuroimaging, postmortem, and genetic studies underlines
the various roles of 5-HT receptor subtypes in the pathogenesis of major depressive …

Human serotonin 5‐HT2C G protein‐coupled receptor homology model from the β2 adrenoceptor structure: Ligand docking and mutagenesis studies

T Córdova‐Sintjago, N Villa, C Canal… - International journal of …, 2012 - Wiley Online Library
Activation of the serotonin (5‐hydroxytryptamine, 5‐HT) 5HT2C G protein‐coupled receptor
(GPCR) is proposed as novel pharmacotherapy for obesity and neuropsychiatric disorders …