keyword
https://read.qxmd.com/read/37789971/lurasidone-for-the-treatment-of-schizophrenia-design-development-and-place-in-therapy
#21
REVIEW
Itaru Miura, Sho Horikoshi, Mizue Ichinose, Yuhei Suzuki, Kenya Watanabe
This review aims to provide a comprehensive overview of the current literature on the drug design, development, and therapy of lurasidone for the treatment of schizophrenia. Lurasidone has antagonistic effects on the dopamine D2 , 5-hydroxytryptamine (5-HT)2A , and 5-HT7 receptors and a partial agonistic effect on the 5-HT1A receptor with low affinities for muscarinic M1 , histamine H1 , and a1 adrenergic receptors. The receptor-binding profile of lurasidone is thought to be associated with fewer side effects such as anticholinergic effects, lipid abnormalities, hyperglycemia, and weight gain...
2023: Drug Design, Development and Therapy
https://read.qxmd.com/read/37783788/repeated-low-doses-of-psilocybin-increase-resilience-to-stress-lower-compulsive-actions-and-strengthen-cortical-connections-to-the-paraventricular-thalamic-nucleus-in-rats
#22
JOURNAL ARTICLE
Kat F Kiilerich, Joe Lorenz, Malthe B Scharff, Nikolaj Speth, Tobias G Brandt, Julia Czurylo, Mengfei Xiong, Naja S Jessen, Agata Casado-Sainz, Vladimir Shalgunov, Celia Kjaerby, Grzegorz Satała, Andrzej J Bojarski, Anders A Jensen, Matthias M Herth, Paul Cumming, Agnete Overgaard, Mikael Palner
Psilocybin (a classic serotonergic psychedelic drug) has received appraisal for use in psychedelic-assisted therapy of several psychiatric disorders. A less explored topic concerns the use of repeated low doses of psychedelics, at a dose that is well below the psychedelic dose used in psychedelic-assisted therapy and often referred to as microdosing. Psilocybin microdose users frequently report increases in mental health, yet such reports are often highly biased and vulnerable to placebo effects. Here we establish and validate a psilocybin microdose-like regimen in rats with repeated low doses of psilocybin administration at a dose derived from occupancy at rat brain 5-HT2A receptors in vivo...
September 2023: Molecular Psychiatry
https://read.qxmd.com/read/37781977/an-adult-drosophila-glioma-model-to-highlight-metabolic-dysfunctions-and-evaluate-the-role-of-the-serotonin-5-ht-7-receptor-as-a-potential-therapeutic-target
#23
JOURNAL ARTICLE
Marylène Bertrand, Frédéric Szeremeta, Nadège Hervouet-Coste, Vincent Sarou-Kanian, Céline Landon, Séverine Morisset-Lopez, Martine Decoville
Gliomas account for 50% of brain cancers and are therefore the most common brain tumors. Molecular alterations involved in adult gliomas have been identified and mainly affect tyrosine kinase receptors with amplification and/or mutation of the epidermal growth factor receptor (EGFR) and its associated signaling pathways. Several targeted therapies have been developed, but current treatments remain ineffective for glioblastomas, the most severe forms. Thus, it is a priority to identify new pharmacological targets...
November 2023: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://read.qxmd.com/read/37641989/amisulpride-decreases-tau-protein-hyperphosphorylation-in-the-brain-of-oxys-rats
#24
JOURNAL ARTICLE
Camilla A Molobekova, Elena M Kondaurova, Tatiana V Ilchibaeva, Alexander Ya Rodnyy, Natalia A Stefanova, Nataliya G Kolosova, Vladimir S Naumenko
AIM: In this study, OXYS rats of three ages (1, 3, and 6 months), a proven model of Alzheimer's disease (AD), at various stages of disease progression were used to thoroughly study the effects of amisulpride on behavior and tau protein phosphorylation. BACKGROUND: With the growing number of patients with AD, the problem of finding a cure is very acute. Neurodegeneration in AD has various causes, one of which is hyperphosphorylation of tau protein. OBJECTIVE: This study aimed to investigate whether amisulpride would affect pathological tau phosphorylation in AD...
August 28, 2023: Current Alzheimer Research
https://read.qxmd.com/read/37637561/the-effects-of-serotonin-receptor-type-7-modulation-on-bowel-sensitivity-and-smooth-muscle-tone-in-patients-with-irritable-bowel-syndrome
#25
REVIEW
Usama Osman, Abishek Latha Kumar, Aishwarya Sadagopan, Anas Mahmoud, Maha Begg, Mawada Tarhuni, Monique N Fotso, Natalie A Gonzalez, Raghavendra R Sanivarapu
Irritable bowel syndrome (IBS) is a gut-brain disorder involving alterations in intestinal sensitivity and motility. Currently, IBS has no cure, and treatment focuses on the management of symptoms. The diverse, and sometimes contradictory, collections of symptoms reported across the different subtypes of IBS make treatment, as well as diagnosis, difficult for physicians. All subtypes of IBS have one symptom in common: abdominal pain caused by differences in the level of visceral sensitivity. Though current research on this topic is in its infancy, some researchers have proven, through experimental studies, that 5-hydroxytryptamine (serotonin) receptor type 7 (5-HT7) affects both visceral sensitivity and smooth muscle tone in the bowel...
July 2023: Curēus
https://read.qxmd.com/read/37631373/anticholinesterase-and-serotoninergic-evaluation-of-benzimidazole-carboxamides-as-potential-multifunctional-agents-for-the-treatment-of-alzheimer-s-disease
#26
JOURNAL ARTICLE
Daria A Belinskaia, Polina A Voronina, Denis V Krivorotov, Richard O Jenkins, Nikolay V Goncharov
The etiology and pathogenesis of Alzheimer's disease are multifactorial, so one of the treatment strategies is the development of the drugs that affect several targets associated with the pathogenesis of the disease. Within this roadmap, we investigated the interaction of several substituted 1,3-dihydro-2-oxo-1 H -benzimidazol-2-ones with their potential molecular targets: cholinesterases (ChE) and three types of the Gs -protein-coupled serotonin receptors (5-HTR) 5-HT6 , 5-HT4 and 5-HT7 (5-HT4 R, 5-HT6 R and 5-HT7 R, respectively)...
August 19, 2023: Pharmaceutics
https://read.qxmd.com/read/37603260/lysergic-acid-diethylamide-lsd-for-the-treatment-of-anxiety-disorders-preclinical-and-clinical-evidence
#27
REVIEW
Antonio Inserra, Alexandre Piot, Danilo De Gregorio, Gabriella Gobbi
Anxiety disorders (ADs) represent the sixth leading cause of disability worldwide, resulting in a significant global economic burden. Over 50% of individuals with ADs do not respond to standard therapies, making the identification of more effective anxiolytic drugs an ongoing research priority. In this work, we review the preclinical literature concerning the effects of lysergic acid diethylamide (LSD) on anxiety-like behaviors in preclinical models, and the clinical literature on anxiolytic effects of LSD in healthy volunteers and patients with ADs...
September 2023: CNS Drugs
https://read.qxmd.com/read/37574491/towards-the-convergent-therapeutic-potential-of-gpcrs-in-autism-spectrum-disorders
#28
REVIEW
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crepieux, Lucie P Pellissier
Autism spectrum disorders (ASD) are diagnosed in 1/100 children worldwide, based on two core symptoms, deficits in social interaction and communication and stereotyped behaviours. G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors that transduce extracellular signals to convergent intracellular signalling and downstream cellular responses that are commonly dysregulated in ASD. Despite hundreds of GPCRs being expressed in the brain, only 23 are genetically associated with ASD according to the Simons Foundation Autism Research Initiative (SFARI) gene database: oxytocin OTR, vasopressin V1A , V1B , metabotropic glutamate mGlu5 , mGlu7 , GABAB2 , dopamine D1 , D2 , D3 , serotoninergic 5-HT1B , β2 -adrenoceptor, cholinergic M3 , adenosine A2A , A3 , angiotensin AT2 , cannabinoid CB1 , chemokine CX3 CR1, orphan GPR37, GPR85 and olfactory OR1C1, OR2M4, OR2T10, OR52M1...
August 13, 2023: British Journal of Pharmacology
https://read.qxmd.com/read/37567058/synthesis-computational-and-experimental-pharmacological-studies-for-thio-ether-triazine-5-ht-6-r-ligands-with-noticeable-action-on-ache-bche-and-chalcogen-dependent-intrinsic-activity-in-search-for-new-class-of-drugs-against-alzheimer-s-disease
#29
JOURNAL ARTICLE
Kinga Czarnota-Łydka, Sylwia Sudoł-Tałaj, Katarzyna Kucwaj-Brysz, Rafał Kurczab, Grzegorz Satała, Modesto de Candia, Francesco Samarelli, Cosimo Damiano Altomare, Alessia Carocci, Alexia Barbarossa, Ewa Żesławska, Monika Głuch-Lutwin, Barbara Mordyl, Monika Kubacka, Natalia Wilczyńska-Zawal, Magdalena Jastrzębska-Więsek, Anna Partyka, Nadia Khan, Małgorzata Więcek, Wojciech Nitek, Ewelina Honkisz-Orzechowska, Gniewomir Latacz, Anna Wesołowska, Antonio Carrieri, Jadwiga Handzlik
Alzheimer's disease is becoming a growing problem increasing at a tremendous rate. Serotonin 5-HT6 receptors appear to be a particularly attractive target from a therapeutic perspective, due to their involvement not only in cognitive processes, but also in depression and psychosis. In this work, we present the synthesis and broad biological characterization of a new series of 18 compounds with a unique 1,3,5-triazine backbone, as potent 5-HT6 receptor ligands. The main aim of this research is to compare the biological activity of the newly synthesized sulfur derivatives with their oxygen analogues and their N-demethylated O- and S-metabolites obtained for the first time...
July 30, 2023: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/37519001/cognitive-effects-of-lurasidone-and-cariprazine-a-mini-systematic-review
#30
JOURNAL ARTICLE
Miriam Olivola, Nicola Bassetti, Serena Parente, Vincenzo Arienti, Serena Chiara Civardi, Pietro Alessandro Topa, Natascia Brondino
BACKGROUND: Cognitive deficits are associated with schizophrenia and show a progressive worsening, often being unresponsive to treatment. New antipsychotic molecules acting as antagonist at the serotoninergic 5-hydroxytryptamine receptor 7 (e.g. lurasidone) or partial agonists at dopamine D3 receptor (e.g. cariprazine) could have an impact on cognition in this patient group. OBJECTIVE: The aim of the systematic review is to explore the efficacy of lurasidone and cariprazine in improving cognition in both animal models and human studies...
July 27, 2023: Current Neuropharmacology
https://read.qxmd.com/read/37509503/serotonergic-modulation-of-neurovascular-transmission-a-focus-on-prejunctional-5-ht-receptors-mechanisms
#31
REVIEW
Abimael González-Hernández, Bruno A Marichal-Cancino, Antoinette MaassenVanDenBrink, Carlos M Villalón
5-Hydroxytryptamine (5-HT), or serotonin, plays a crucial role as a neuromodulator and/or neurotransmitter of several nervous system functions. Its actions are complex, and depend on multiple factors, including the type of effector or receptor activated. Briefly, 5-HT can activate: (i) metabotropic (G-protein-coupled) receptors to promote inhibition (5-HT1 , 5-HT5 ) or activation (5-HT4 , 5-HT6 , 5-HT7 ) of adenylate cyclase, as well as activation (5-HT2 ) of phospholipase C; and (ii) ionotropic receptor (5-HT3 ), a ligand-gated Na+ /K+ channel...
June 29, 2023: Biomedicines
https://read.qxmd.com/read/37367324/identification-and-expression-profiling-of-the-5-ht-receptor-gene-in-harmonia-axyridis
#32
JOURNAL ARTICLE
Qiqi Zhang, Yifang Chang, Changying Zheng, Lijuan Sun
It has been found that 5-hydroxytryptamine (5-HT) modulates the feeding of some insects, and this phenomenon was found in Harmonia axyridis (Pallas) by our previous study. An understanding of the 5-HT system in this beetle is helpful for utilizing 5-HT to modulate its predation to improve biological control efficiency, especially in greenhouses in winter in north China. This is because 5-HT influences diapause in insects by modulating the synthesis and release of prothoracic hormone (PTTH) and, therefore, influences feeding...
May 31, 2023: Insects
https://read.qxmd.com/read/37360419/enantiomeric-separation-absolute-configuration-by-x-ray-crystallographic-analysis-and-functional-evaluation-of-enantiomers-of-the-dual-ligand-sya0340-at-5-ht-1a-and-5-ht-7a-receptors
#33
JOURNAL ARTICLE
Barbara A Bricker, Chandrashekhar Voshavar, Edem K Onyameh, Uma M Gonela, Xinsong Lin, Tracy L Swanson, Laura B Kozell, Jennifer L Schmachtenberg, Shelley H Bloom, Aaron J Janowsky, Seth Y Ablordeppey
We have previously identified 5-chloro-2-methyl-2-(3-(4-(pyridin-2-yl)piperazin-1-yl)propyl)-2,3-dihydro-1 H -inden-1-one (SYA0340) as a dual 5-HT1A and 5-HT7 receptor ligand, and we posited such ligands might find utility in the treatment of various CNS related illnesses including cognitive and anxiolytic impairments. However, SYA0340 has a chiral center and its enantiomers may confound the readouts for their functional characteristics. Thus, in this study, we resynthesized SYA0340, separated the enantiomers, identified the absolute configurations, and evaluated their binding affinities and functional characteristics at both the 5-HT1A and 5-HT7A receptors...
June 20, 2023: ACS Omega
https://read.qxmd.com/read/37342875/serotonin-5-ht-7-receptor-slows-down-the-g-s-protein-a-single-molecule-perspective
#34
JOURNAL ARTICLE
Aleš Petelák, Nevin A Lambert, Alexey Bondar
The 5-hydroxytryptamine (serotonin) receptor type 7 (5-HT7 R) is a G protein-coupled receptor (GPCR) present primarily in the nervous system and gastrointestinal tract, where it regulates mood, cognition, digestion, and vasoconstriction. 5-HT7 R has previously been shown to bind to its cognate stimulatory Gs protein in the inactive state. This phenomenon, termed inverse coupling, is thought to counteract the atypically high intrinsic activity of 5-HT7 R. However, it is not clear how active and inactive 5-HT7 receptors affect the mobility of the Gs protein in the plasma membrane...
June 21, 2023: Molecular Biology of the Cell
https://read.qxmd.com/read/37339717/the-5-ht-7-receptors-in-the-vlo-contribute-to-the-development-of-morphine-induced-behavioral-sensitization-in-rats
#35
JOURNAL ARTICLE
Jing-Si Yang, Fei-Fei Gao, Xi-Xi Yang, Feng Liang, Zhuo-Jin Yang, Jie Chen, Yu-Xiang Zhang, Chun-Xia Yan
The 5-hydroxytryptamine 7 receptor (5-HT7 R) is one of the most recently cloned serotonin receptors which have been implicated in many physiological and pathological processes including drug addiction. Behavioral sensitization is the progressive process during which re-exposure to drugs intensified the behavioral and neurochemical responses to drugs. Our previous study has demonstrated that the ventrolateral orbital cortex (VLO) is critical for morphine-induced reinforcing effect. The aim of the present study was to investigate the effect of 5-HT7 Rs in the VLO on morphine-induced behavioral sensitization and their underlying molecular mechanisms...
June 18, 2023: Neurochemistry International
https://read.qxmd.com/read/37333908/recommendations-for-selection-and-adaptation-of-rating-scales-for-clinical-studies-of-rapid-acting-antidepressants
#36
REVIEW
Christian Yavorsky, Elizabeth Ballard, Mark Opler, Jan Sedway, Steven D Targum, William Lenderking
The novel mechanisms of action (MOA) derived from some recently introduced molecular targets have led to regulatory approvals for rapid acting antidepressants (RAADs) that can generate responses within hours or days, rather than weeks or months. These novel targets include the N-methyl-D-glutamate receptor antagonist ketamine, along with its enantiomers and various derivatives, and the allosteric modulators of gamma-aminobutyric acid (GABA) receptors. There has also been a strong resurgence in interest in psychedelic compounds that impact a range of receptor sites including D1, 5-HT7, KOR, 5-HT5A, Sigma-1, NMDA, and BDNF...
2023: Frontiers in Psychiatry
https://read.qxmd.com/read/37270968/antidepressant-effects-of-p-coumaric-acid-isolated-from-vaccinium-bracteatum-leaves-extract-on-chronic-restraint-stress-mouse-model-and-antagonism-of-serotonin-6-receptor-in-vitro
#37
JOURNAL ARTICLE
Dool-Ri Oh, Chulyung Choi, Moon Jong Kim, Bo Yeong Mun, Haeju Ko, Kyo-Nyeo Oh, Ara Jo, Jin Young Kim, Donghyuck Bae
BACKGROUND: Vaccinium bracteatum Thunb. leaves (VBL) are used in traditional herbal medicines to treat various biological diseases. p-coumaric acid (CA), the main active component of VBL, has neuroprotective effects against corticosterone-induced damage in vitro. However, the effects of CA on immobility induced by chronic restraint stress (CRS) in a mouse model and 5-HT receptor activity have not been investigated. HYPOTHESIS/PURPOSE: We investigated the antagonistic effects of VBL, NET-D1602, and the three components of Gαs protein-coupled 5-HT receptors...
May 10, 2023: Phytomedicine
https://read.qxmd.com/read/37259325/novel-multimodal-salicylamide-derivative-with-antidepressant-like-anxiolytic-like-antipsychotic-like-and-anti-amnesic-activity-in-mice
#38
JOURNAL ARTICLE
Elżbieta Żmudzka, Klaudia Lustyk, Monika Głuch-Lutwin, Małgorzata Wolak, Jolanta Jaśkowska, Marcin Kołaczkowski, Jacek Sapa, Karolina Pytka
Depression, anxiety, and schizophrenia may coexist in psychiatric patients. Moreover, these disorders are very often associated with cognitive impairments. However, pharmacotherapy of these conditions remains challenging due to limited drug effectiveness or numerous side effects. Therefore, there is an urgent need to develop novel multimodal compounds that can be used to treat depression, anxiety, and schizophrenia, as well as memory deficits. Thus, this study aimed to evaluate the potential antidepressant-like, anxiolytic-like, antipsychotic-like effects, and anti-amnesic properties, of the novel arylpiperazine derivative of salicylamide, JJGW07, with an affinity towards serotonin 5-HT1A , 5-HT2A , and 5-HT7 and dopamine D2 receptors...
January 24, 2023: Pharmaceuticals
https://read.qxmd.com/read/37240731/gut-microbiota-derived-short-chain-fatty-acids-novel-regulators-of-intestinal-serotonin-transporter
#39
JOURNAL ARTICLE
Berta Buey, Ana Forcén, Laura Grasa, Elena Layunta, Jose Emilio Mesonero, Eva Latorre
Serotonin (5-HT) is a key neurotransmitter synthesized both in the gut and the central nervous system. It exerts its signaling through specific receptors (5-HTR), which regulate numerous behaviors and functions such as mood, cognitive function, platelet aggregation, gastrointestinal motility, and inflammation. Serotonin activity is determined mainly by the extracellular availability of 5-HT, which is controlled by the serotonin transporter (SERT). Recent studies indicate that, by activation of innate immunity receptors, gut microbiota can modulate serotonergic signaling by SERT modulation...
April 26, 2023: Life
https://read.qxmd.com/read/37204759/5-ht-7-receptors-mediate-dilation-of-rat-cremaster-muscle-arterioles-in-vivo
#40
JOURNAL ARTICLE
William F Jackson, Armond Daci, Janice M Thompson, Gregory D Fink, Stephanie W Watts
OBJECTIVE: Serotonin (5-HT) infusion in vivo causes hypotension and a fall in total peripheral resistance. However, the vascular segment and the receptors that mediate this response remain in question. We hypothesized that 5-HT7 receptors mediate arteriolar dilation to 5-HT in skeletal muscle microcirculation. METHODS: Cremaster muscles of isoflurane-anesthetized male Sprague-Dawley rats were prepared for in vivo microscopy of third- and fourth-order arterioles and superfused with physiological salt solution at 34°C...
May 19, 2023: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
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