Journal ArticleDOI
Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders.
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TLDR
In this article, a new generation of highly selective, efficacious and druggable biased agonists have been identified which exhibit increased affinity at 5-HT1A receptors and new profiles of cellular signaling bias, notably for β-arrestin recruitment versus pERK.About:
This article is published in Pharmacology & Therapeutics.The article was published on 2021-06-24. It has received 22 citations till now. The article focuses on the topics: Functional selectivity & Serotonergic.read more
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Biased β-Agonists Favoring Gs over β-Arrestin for Individualized Treatment of Obstructive Lung Disease
TL;DR: It is shown how combinatorial methods with a 40 million compound agnostic library led to a new class of biased β-agonists that do not desensitize, providing an opportunity to personalize therapy in patients who experience poor efficacy or adverse effects from traditional balanced agonists.
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Molecular Imaging in Parkinsonian Disorders—What’s New and Hot?
TL;DR: The role of molecular imaging in the context of disease-modifying interventions to follow neurodegeneration, ensure stratification, and target engagement in clinical trials is reviewed and the most recent advances in molecular imaging for the diagnosis, prognosis, and mechanistic understanding of parkinsonian disorders are reviewed.
Journal ArticleDOI
The pathophysiology of Post SSRI Sexual Dysfunction - Lessons from a case study.
TL;DR: In this paper , a 55-year-old male patient developed symptoms of low libido, delayed ejaculation, erectile dysfunction, brain zaps, overactive bladder and urinary inconsistency after discontinuation of the SNRI venlafaxine.
Journal ArticleDOI
Synthesis, Docking Studies and Pharmacological Evaluation of Serotoninergic Ligands Containing a 5-Norbornene-2-Carboxamide Nucleus
Rose Sparaco,Ewa Kędzierska,Agnieszka Kaczor,Anna Bielenica,Elisa Magli,Beatrice Severino,Angela Corvino,Ewa Gibula-Tarlowska,Jolanta Kotlinska,G. Andreozzi,Paolo Luciano,Elisa Perissutti,Francesco Frecentese,Marcello Casertano,Anna Lesniak,Magdalena Bujalska-Zadrożny,Małgorzata Oziębło,Raffaele Capasso,Vincenzo Santagada,Giuseppe Caliendo,Ferdinando Fiorino +20 more
TL;DR: Norbo-4 and Norbo-18 were the most active and promising derivatives for the serotonin receptor considered in this study and molecular docking studies were performed to rationalize the obtained results.
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Acute and Repeated Administration of NLX-101, a Selective Serotonin-1A Receptor Biased Agonist, Reduces Audiogenic Seizures in Developing Fmr1 Knockout Mice
TL;DR: In this article , a selective and post-synaptic 5-HT1A receptor biased agonist, 3-Chloro-4fluorophenyl-[4-fluoro-4]-4-methyl-methyl)amino]methyl]piperidin-1-yl] methanone (NLX-101, 0.6, 1.8 or 2.4 mg/kg, i.p., was administered to Fmr1 KO mice 15 min before seizure induction.
References
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Heiko Braak,Eva Braak +1 more
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Validation of open:closed arm entries in an elevated plus-maze as a measure of anxiety in the rat.
TL;DR: A novel test for the selective identification of anxiolytic and anxiogenic drug effects in the rat is described, using an elevated + -maze consisting of two open arms and two enclosed arms, which showed that behaviour on the maze was not clearly correlated either with exploratory head-dipping or spontaneous locomotor activity.
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A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.
TL;DR: In this paper, a ternary complex model was used to fit the data with high accuracy under conditions where the ligand used is either a full or a partial agonist and where the system is altered by the addition of guanine nucleotide or after treatment with group-specific reagents.
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A mouse Mecp2-null mutation causes neurological symptoms that mimic rett syndrome
TL;DR: The overlapping delay before symptom onset in humans and mice raises the possibility that stability of brain function, not brain development per se, is compromised by the absence of MeCP2, and generates mice lacking Mecp2 using Cre-loxP technology.
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Chronic mild stress-induced anhedonia : a realistic animal model of depression
TL;DR: The validity of chronic mild stress-induced anhedonia as an animal model of depression is reviewed, and the evidence that changes in hedonic responsiveness in this model are mediated by changes in the sensitivity of dopamine D2 receptors in the nucleus accumbens is reviewed.