Investigation of the 2,5-Dimethoxy Motif in Phenethylamine Serotonin 2A Receptor Agonists

2020 ◽  
Vol 11 (9) ◽  
pp. 1238-1244
Author(s):  
Emil Marcher-Rørsted ◽  
Adam L. Halberstadt ◽  
Adam K. Klein ◽  
Muhammad Chatha ◽  
Simon Jademyr ◽  
...  
Keyword(s):  
Serotonin 2A Receptor ◽  
Receptor Agonists ◽  
Serotonin 2A

scholarly journals The mGlu2/3 Receptor Agonists LY354740 and LY379268 Differentially Regulate Restraint-Stress-Induced Expression of c-Fos in Rat Cerebral Cortex

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
M. M. Menezes ◽  
M. A. Santini ◽  
M. J. Benvenga ◽  
G. J. Marek ◽  
K. M. Merchant ◽  
...  
Keyword(s):  
Restraint Stress ◽  
Early Gene ◽  
Induced Expression ◽  
Serotonin 2A Receptor ◽  
Receptor Agonists ◽  
Metabotropic Glutamate ◽  
Excitatory Transmission ◽  
Fos Expression ◽  
Serotonin 2A

Metabotropic glutamate 2/3 (mGlu2/3) receptors have emerged as potential therapeutic targets due to the ability of mGlu2/3 receptor agonists to modulate excitatory transmission at specific synapses. LY354740 and LY379268 are selective and potent mGlu2/3 receptor agonists that show both anxiolytic- and antipsychotic-like effects in animal models. We compared the efficacy of LY354740 and LY379268 in attenuating restraint-stress-induced expression of the immediate early gene c-Fos in the rat prelimbic (PrL) and infralimbic (IL) cortex. LY354740 (10 and 30 mg/kg, i.p.) showed statistically significant and dose-related attenuation of stress-induced increase in c-Fos expression, in the rat cortex. By contrast, LY379268 had no effect on restraint-stress-induced c-Fos upregulation (0.3–10 mg/kg, i.p.). Because both compounds inhibit serotonin 2A receptor (5-HT2AR)-induced c-Fos expression, we hypothesize that LY354740 and LY379268 have different in vivo properties and that 5-HT2AR activation and restraint stress induce c-Fos through distinct mechanisms.

Genetic dysfunction of serotonin 2A receptor hampers response to antidepressant drugs: A translational approach

2016 ◽  
Vol 105 ◽  
pp. 142-153 ◽  
Author(s):  
Gaël Qesseveur ◽  
Anne Cécile Petit ◽  
Hai Thanh Nguyen ◽  
Lionel Dahan ◽  
Romain Colle ◽  
...  
Keyword(s):  
Antidepressant Drugs ◽  
Serotonin 2A Receptor ◽  
Translational Approach ◽  
Serotonin 2A

Enhanced prefrontal serotonin 2A receptor signaling in the subchronic phencyclidine mouse model of schizophrenia

2013 ◽  
Vol 91 (5) ◽  
pp. 634-641 ◽  
Author(s):  
Martin A. Santini ◽  
Cecilia Ratner ◽  
Susana Aznar ◽  
Anders B. Klein ◽  
Gitte M. Knudsen ◽  
...  
Keyword(s):  
Mouse Model ◽  
Receptor Signaling ◽  
Serotonin 2A Receptor ◽  
Serotonin 2A

scholarly journals Serotonin 2A receptor disulfide bridge integrity is crucial for ligand binding to different signalling states but not for its homodimerization

2017 ◽  
Vol 815 ◽  
pp. 138-146 ◽  
Author(s):  
Alba Iglesias ◽  
Marta Cimadevila ◽  
Rocío Ailim de la Fuente ◽  
María Martí-Solano ◽  
María Isabel Cadavid ◽  
...  
Keyword(s):  
Ligand Binding ◽  
Disulfide Bridge ◽  
Serotonin 2A Receptor ◽  
Serotonin 2A

scholarly journals Acute serotonin 2A receptor blocking alters the processing of fearful faces in the orbitofrontal cortex and amygdala

2013 ◽  
Vol 27 (10) ◽  
pp. 903-914 ◽  
Author(s):  
Bettina Hornboll ◽  
Julian Macoveanu ◽  
James Rowe ◽  
Rebecca Elliott ◽  
Olaf B Paulson ◽  
...  
Keyword(s):  
Orbitofrontal Cortex ◽  
Serotonin 2A Receptor ◽  
Receptor Blocking ◽  
Fearful Faces ◽  
Serotonin 2A

scholarly journals Association analysis between the C516T polymorphism in the 5-HT2A receptor gene and schizophrenia

2007 ◽  
Vol 65 (1) ◽  
pp. 11-14 ◽  
Author(s):  
Vivian Bertola ◽  
Quirino Cordeiro ◽  
Stevin Zung ◽  
Elisabete Cristina Miracca ◽  
Homero Vallada
Keyword(s):  
Atypical Antipsychotics ◽  
Receptor Gene ◽  
Epidemiological Studies ◽  
Case Control ◽  
Psychotic Symptoms ◽  
Serotonin 2A Receptor ◽  
Brazilian Sample ◽  
Control Approach ◽  
Serotonergic Drugs ◽  
Serotonin 2A

Data from epidemiological studies have demonstrated that genetics is an important risk factor for schizophrenia. Disturbances of serotonergic brain pathways have been implicated in the pathophysiology of schizophrenia. Some studies have suggested that the efficacy of atypical antipsychotics on schizophrenia treatment may be related to the serotonin 2A receptor (5-HT2A), and that serotonergic drugs may induce psychotic symptoms. Thus, the aim of this study was to investigate the association between the C516T polymorphism and schizophrenia in a Brazilian population composed by 246 patients and 315 healthy matched controls in a case-control approach. No statistically differences were observed in allelic (chi2=1.77, 1d.f., p=0.18) or genotypic (chi2=1.69, 2d.f., p=0.42) distributions between cases and controls. The results suggest that the C516T polymorphism of the 5-HT2A receptor gene is not related to the susceptibility for schizophrenia in our Brazilian sample.

Association of Serotonin 2A Receptor and Lack of Association of CYP1A2 Gene Polymorphism with Tardive Dyskinesia in a Turkish Population

2007 ◽  
Vol 26 (8) ◽  
pp. 527-531 ◽  
Author(s):  
Omer Boke ◽  
Sezgin Gunes ◽  
Nurten Kara ◽  
Servet Aker ◽  
Ahmet Rifat Sahin ◽  
...  
Keyword(s):  
Gene Polymorphism ◽  
Tardive Dyskinesia ◽  
Turkish Population ◽  
Serotonin 2A Receptor ◽  
Serotonin 2A

scholarly journals Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy

2018 ◽  
Vol 10 (3) ◽  
pp. 178-195 ◽  
Author(s):  
Lin Cao ◽  
Jizheng Chen ◽  
Yaxin Wang ◽  
Yuting Yang ◽  
Jie Qing ◽  
...  
Keyword(s):  
Chemical Biology ◽  
Serotonin 2A Receptor ◽  
Serotonin 2A

P.107 Common HTR2A variants and 5-HTTLPR are not associated with in-vivo serotonin 2A receptor binding in healthy humans

2020 ◽  
Vol 31 ◽  
pp. S6-S7
Author(s):  
M. Spies ◽  
A. Nasser ◽  
B. Ozenne ◽  
P.S. Jensen ◽  
G.M. Knudsen ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Serotonin 2A Receptor ◽  
Healthy Humans ◽  
Serotonin 2A
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