Antagonist Functional Selectivity: 5-HT2A Serotonin Receptor Antagonists Differentially Regulate 5-HT2A Receptor Protein Level In Vivo [PDF]
The Journal of Pharmacology and Experimental Therapeutics, 2011 Dysregulation of the 5-HT2A receptor is implicated in both the etiology and treatment of schizophrenia. Although the essential role of 5-HT2A receptors in atypical antipsychotic drug actions is widely accepted, the contribution of 5-HT2A down-regulation to their efficacy is not known.
Prem N, Yadav +3 more
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Genotype-Dependent Difference in 5-HT2C Receptor-Induced Hypolocomotion: Comparison with 5-HT2A Receptor Functional Activity [PDF]
Neural Plasticity, 2015 In the present study behavioral effects of the 5-HT2C serotonin receptor were investigated in different mouse strains. The 5-HT2C receptor agonist MK-212 applied intraperitoneally induced significant dose-dependent reduction of distance traveled in the ...
Darya V. Bazovkina +3 more
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Overcoming Depression with 5-HT2A Receptor Ligands [PDF]
Int J Mol Sci, 2023 Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents.
Agata Zięba +3 more
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5-HT2A Receptor Gene Polymorphisms and Irritable Bowel Syndrome
Journal of Clinical Gastroenterology, 2011 The aim of the study was to investigate the potential association between single nucleotide polymorphisms of the 5-HT2A receptor gene and susceptibility to irritable bowel syndrome (IBS) in the Greek population.Serotonin [5-hydroxytryptamine (5-HT)] is the main mediator involved in the pathophysiology of IBS.
Markoutsaki, T. +4 more
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Biased signaling via serotonin 5-HT2A receptor: From structural aspects to in vitro and in vivo pharmacology [PDF]
Acta Pharmaceutica Sinica BG protein-coupled receptors (GPCRs) represent key drug targets, with approximately 30%–40% of all medications acting on these receptors. Recent advancements have uncovered the complexity of GPCR signaling, including biased signaling, which allows ...
Michał K. Jastrzębski +11 more
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Impulsive traits and 5-HT2A receptor promoter polymorphism in alcohol dependents: Possible association but no influence of personality disorders [PDF]
, 2001 Objective: Impulsive behavior in alcoholics puts them at serious risk of severer course of disease and has been related to the serotonergic neurotransmission dysfunction.
Bondy, Brigitta +4 more
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Pharmacology of novel psychoactive substances [PDF]
, 2016 This PhD work consists of an in vitro and in vivo part. In the in vivo part, we investigated the role of dopamine in the acute clinical effects of 3,4-methylenedioxymethamphetamine (MDMA, “ecstasy”) in healthy human subjects.
Rickli, Anna
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Journal of Pharmacological Sciences, 2018 We examined whether combination treatment with doxorubicin and cyclophosphamide, a traditional chemotherapy for breast cancer, induced anxiety-like behavior in rats.
Yuka Nakamura +8 more
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Frontiers in Pharmacology, 2022 Various forms of traumatic brain injury (TBI) are a leading cause of disability in the United States, with the generation of neuropsychiatric complications such as depression, anxiety, social dysfunction, and suicidality being common comorbidities ...
Sean M. Collins +9 more
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Development of novel chiral capillary electrophoresis methods for the serotonin receptor (5-HT2A) antagonist MDL 100,907 (volinanserin) and for its key intermediate compound [PDF]
, 2014 Enantioselective capillary electrophoretic methods were elaborated for the determination of the enantiomeric purity of (R)-MDL 100,907 and its preparatively resolved key intermediate compound during the synthesis route. The pKa values of the intermediate
Palkó, Roberta +3 more
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