keyword
https://read.qxmd.com/read/38126116/il-6-expression-suppressing-lactobacillus-reuteri-strains-alleviate-gut-microbiota-induced-anxiety-and-depression-in-mice
#1
JOURNAL ARTICLE
Xiaoyang Ma, Jeong-Woo Shin, Jae-Hyun Cho, Seung-Won Han, Dong-Hyun Kim
Fecal microbiota transplantation from patients with depression/inflammatory bowel disease (PDI) causes depression with gut inflammation in mice. Here, we investigated the effects of six Lactobacillus reuteri strains on BDNF, serotonin, and IL-6 expression in neuronal or macrophage cells and PDI fecal microbiota-cultured microbiota (PcM)-induced depression in mice. Of these strains, L6 most potently increased BDNF and serotonin levels in corticosterone-stimulated SH-SY5Ycells and PC12 cells, followed by L3. L6 most potently decreased IL-6 expression in LPS-stimulated macrophages...
December 20, 2023: Letters in Applied Microbiology
https://read.qxmd.com/read/37519001/cognitive-effects-of-lurasidone-and-cariprazine-a-mini-systematic-review
#2
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/37482048/synthesis-computational-simulations-and-biological-evaluation-of-new-dual-5ht-1a-5ht-7-receptor-ligands-based-on-purine-2-6-dione-scaffold
#3
JOURNAL ARTICLE
Agnieszka Zagórska, Anna Partyka, Magdalena Jastrzębska-Więsek, Anna Czopek, Monika Fryc, Agata Siwek, Monika Głuch-Lutwin, Barbara Mordyl, Anna Maślanka, Anna Jaromin, Rafał Kurczab
The new dual 5HT1A /5HT7 receptor ligands were designed based on the purine-2,6-dione scaffold with the fluorine atom. Twenty-one new derivatives were synthesized, and their structure-activity relationship was summarized. Compound 11 (7-(2-(3-fluorophenyl)-2-oxoethyl)-8-((4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)amino)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione) showed the highest affinity to 5HT1A R and 5HT7 R, and was the most potent antagonist of 5-HT1A R (Kb  = 0.26 ± 0.1 nM) which activity can be to reference compound NAN-190 (Kb  = 0...
July 19, 2023: Bioorganic Chemistry
https://read.qxmd.com/read/37249676/biological-evaluation-and-binding-mechanism-of-5-ht-7-specific-arylpiperazinyl-alkyl-benzothiazolone-radiobiology-and-photo-physical-studies
#4
JOURNAL ARTICLE
Neelam Kumari, Deepika Singh, Priya Singh, Akanksha Mishra, Chandraprakash Gond, Himanshu Ojha, Anjani Kumar Tiwari
Diversely substituted methoxy derivatives of arylpiperazinyl-alkyl benzothiazolone has been evaluated as specific probe for 5HT7 . To determine the best methoxy derivative for 5HT7 receptor affinity, we synthesised a number of 2-benzothiazolone arylalkyl piperazine derivatives. In-vitro/vivo studies with C-2 substituted [11 C]ABT showed 5HT7 specific binding. The radiochemical purity of [11 C]ABT was found to be more than 99% with radiochemical stability persistence for more than 1.5 hr at 25 °C. The interaction of BSA and ABT has been analysed by photophysical studies for better understanding of properties such as adsortion, distribution, metabolism and elemination (ADME)...
May 30, 2023: Journal of Fluorescence
https://read.qxmd.com/read/37065917/evaluating-the-effect-of-r-baclofen-and-lp-211-on-autistic-behavior-of-the-btbr-and-fmr1-ko-mouse-models
#5
JOURNAL ARTICLE
Shirin Sharghi, Stefanie Flunkert, Magdalena Daurer, Roland Rabl, Boris Philippe Chagnaud, Marcello Leopoldo, Enza Lacivita, Birgit Hutter-Paier, Manuela Prokesch
INTRODUCTION: Autism spectrum disorder (ASD) is a persistent neurodevelopmental condition characterized by two core behavioral symptoms: impaired social communication and interaction, as well as stereotypic, repetitive behavior. No distinct cause of ASD is known so far; however, excitatory/inhibitory imbalance and a disturbed serotoninergic transmission have been identified as prominent candidates responsible for ASD etiology. METHODS: The GABA B receptor agonist R-Baclofen and the selective agonist for the 5HT7 serotonin receptor LP-211 have been reported to correct social deficits and repetitive behaviors in mouse models of ASD...
2023: Frontiers in Neuroscience
https://read.qxmd.com/read/36535771/subtype-specific-roles-of-ellipsoid-body-ring-neurons-in-sleep-regulation-in-drosophila
#6
JOURNAL ARTICLE
Wei Yan 闫薇, Hai Lin 林海, Junwei Yu 于俊伟, Timothy D Wiggin, Litao Wu 伍立桃, Zhiqiang Meng 孟志强, Chang Liu 刘畅, Leslie C Griffith
The ellipsoid body (EB) is a major structure of the central complex of the Drosophila melanogaster brain. 22 subtypes of EB ring neurons have been identified based on anatomical and morphological characteristics by light-level microscopy and EM connectomics. A few studies have associated ring neurons with the regulation of sleep homeostasis and structure. However, cell type-specific and population interactions in the regulation of sleep remain unclear. Employing an unbiased thermogenetic screen of EB drivers using female flies, we found: 1) multiple ring neurons are involved in the modulation of amount of sleep and structure in a synergistic manner; 2) analysis of data for ΔP(doze)/ΔP(wake) using a mixed Gaussian model detected 5 clusters of GAL4 drivers which had similar effects on sleep pressure and/or depth: lines driving arousal contained R4m neurons, whereas lines that increased sleep pressure had R3m cells; 3) a general linear model analysis correlating ring cell subtype and activity-dependent changes in sleep parameters across all lines identified several cell types significantly associated with specific sleep effects: R3p was daytime sleep-promoting, and R4m was nighttime wake-promoting; and 4) R3d cells present in 5HT7-GAL4 and in GAL4 lines which exclusively affect sleep structure, were found to contribute to fragmentation of sleep during both day and night...
December 14, 2022: Journal of Neuroscience
https://read.qxmd.com/read/35841422/a-randomized-double-blind-placebo-controlled-phase-1-study-of-the-safety-tolerability-pharmacokinetics-and-pharmacodynamics-of-lb-102-a-selective-dopamine-d-2-3-5-ht-7-inhibitor
#7
RANDOMIZED CONTROLLED TRIAL
Lukasz Biernat, Vincent T Grattan, Mark S Hixon, Zachary Prensky, Andrew R Vaino
LB-102 is an N-methylated analogue of amisulpride under development to treat schizophrenia. LB-102 was evaluated in a Phase 1, double-blind, placebo-controlled, clinical study to evaluate safety and pharmacokinetics. This was a first-in-human study examining single and multiple doses of LB-102 administered orally in 64 healthy volunteers. Dosing in the single ascending dose (SAD) portion of the study was initially planned to be 50, 100, 200, and 400 mg, with doses in the multiple ascending dose (MAD) portion to be determined based on observations in the SAD portion...
September 2022: Psychopharmacology
https://read.qxmd.com/read/35555161/acute-intermittent-hypoxia-preconditioning-elicits-age-and-sex-dependent-changes-in-molecules-known-to-regulate-phrenic-motor-plasticity
#8
JOURNAL ARTICLE
Jayakrishnan Nair, Alexandria B Marciante, Yasin B Seven, Mia N Kelly, Carter Lurk, Jose R Oberto, Gordon S Mitchell
Acute intermittent hypoxia (AIH) elicits a form of respiratory motor plasticity known as phrenic long-term facilitation (pLTF); preconditioning with daily AIH (dAIH) enhances pLTF, demonstrating metaplasticity. Two additional factors impacting pLTF expression are age and sex: whereas moderate AIH-induced pLTF decreases with age in males, it increases in middle aged females. Unfortunately, little is known concerning mechanisms of dAIH preconditioning or age-dependent sexual dimorphism in pLTF. Moderate AIH elicits 2 distinct signaling cascades in phrenic motor neurons initiated by 5HT2A/2B receptors (Q pathway) versus adenosine 2A or 5HT7 receptors (S pathway), respectively...
May 2022: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://read.qxmd.com/read/35553289/serum-estradiol-level-correlates-with-molecules-regulating-phrenic-motoneuron-plasticity
#9
JOURNAL ARTICLE
Carter Lurk, Jay Nair, Alex B Marciante, Gordon S Mitchell
Acute Intermittent Hypoxia (AIH) elicits phrenic long-term facilitation (pLTF), an important model of respiratory motor plasticity. Although moderate AIH-induced pLTF exhibits profound age-dependent sexual dimorphism, little is known concerning the age or sex-dependent changes in molecules regulating the Q or S pathways to phrenic motor facilitation. AIH elicits pLTF via distinct signaling pathways in phrenic motor neurons initiated by 5HT2A/2B (Q pathway) or 5HT7 & Adenosine 2A receptors (S pathway); these pathways interact via powerful crosstalk inhibition...
May 2022: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://read.qxmd.com/read/35016263/influence-of-developmental-nicotine-exposure-on-serotonergic-control-of-breathing-related-motor-output
#10
JOURNAL ARTICLE
Lila Wollman, Andrew Hill, Brady Hasse, Christina Young, Giovanni Hernandez-De La Pena, Richard B Levine, Ralph F Fregosi
Serotonin plays an important role in the development of brainstem circuits that control breathing. Here, we test the hypothesis that developmental nicotine exposure (DNE) alters the breathing-related motor response to serotonin (5HT). Pregnant rats were exposed to nicotine or saline, and brainstem-spinal cord preparations from 1- to 5-day-old pups were studied in a split-bath configuration, allowing drugs to be applied selectively to the medulla or spinal cord. The activity of the fourth cervical ventral nerve roots (C4VR), which contain axons of phrenic motoneurons, was recorded...
March 2022: Developmental Neurobiology
https://read.qxmd.com/read/34497709/vortioxetine-as-a-new-frontier-in-the-treatment-of-chronic-neuropathic-pain-a-review-and-update
#11
REVIEW
Daniela Adamo, Elena Calabria, Noemi Coppola, Giuseppe Pecoraro, Michele Davide Mignogna
Chronic neuropathic pain (CNP) is a disabling medical condition that impairs the health-related quality-of-life of affected patients. A high prevalence of anxiety, depression, sleep disturbance and cognitive impairment has frequently been reported in association with CNP, making the management of this disease complex and often multidisciplinary. Dual-acting agents such as selective serotonin and noradrenalin reuptake inhibitors (SNRIs) are considered particularly useful in the modulation of pain and in treatment of the mood disorders frequently associated with CNP...
2021: Therapeutic Advances in Psychopharmacology
https://read.qxmd.com/read/34015444/5-ht7-receptor-activation-rescues-impaired-synaptic-plasticity-in-an-autistic-like-rat-model-induced-by-prenatal-vpa-exposure
#12
JOURNAL ARTICLE
Maryam Khodaverdi, Mona Rahdar, Shima Davoudi, Razieh Hajisoltani, Zohreh Tavassoli, Zahra Ghasemi, Aeen Ebrahim Amini, Narges Hosseinmardi, Gila Behzadi, Mahyar Janahmadi
Autism spectrum disorder (ASD) is a severe life-long neuropsychiatric disorder. Alterations and imbalance of several neurochemical systems may be involved in ASD pathophysiology, of them, serotonergic neurotransmission dysfunction and deficiency may underlie behavioral abnormalities associated with ASD. However, the functional importance of serotonergic receptors, particularly 5HT7 receptors in ASD pathology remains poorly defined. Serotonin receptor subtype 7 (5-HT7R) plays a direct regulatory role in the development and also for the mature function of the brain, therefore, further studies are necessary to elucidate the role of these receptors in the etiology of autism...
September 2021: Neurobiology of Learning and Memory
https://read.qxmd.com/read/32943849/transdermal-asenapine-in-schizophrenia-a-systematic-review
#13
REVIEW
Brennan Carrithers, Rif S El-Mallakh
BACKGROUND: Asenapine is a novel antipsychotic that has demonstrated efficacy in controlling psychosis in schizophrenia and mania in bipolar illness. It must be administered as a sublingual formulation because it is nearly completely metabolized in the first pass through the liver. Recently, a transdermal formulation of asenapine has been approved for schizophrenia by the Food and Drug Administration. METHODS: A systematic review of transdermal asenapine was done utilizing the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) model...
2020: Patient Preference and Adherence
https://read.qxmd.com/read/31971473/spinal-amp-kinase-activity-differentially-regulates-phrenic-motor-plasticity
#14
JOURNAL ARTICLE
Raphael Rodrigues Perim, Daryl P Fields, Gordon S Mitchell
Acute intermittent hypoxia (AIH) elicits phrenic motor plasticity via multiple distinct cellular mechanisms. With moderate AIH, phrenic motor facilitation (pMF) requires Gq protein-coupled serotonin type 2 receptor activation, ERK MAP kinase activity, and new synthesis of brain-derived neurotrophic factor. In contrast, severe AIH elicits pMF by an adenosine-dependent mechanism that requires exchange protein activated by cAMP, Akt, and mammalian target of rapamycin (mTOR) activity, followed by new tyrosine receptor kinase B protein synthesis; this same pathway is also initiated by Gs protein-coupled serotonin 7 receptors (5-HT7 )...
March 1, 2020: Journal of Applied Physiology
https://read.qxmd.com/read/31226329/differential-modulation-of-courtship-behavior-and-subsequent-aggression-by-octopamine-dopamine-and-serotonin-in-male-crickets
#15
JOURNAL ARTICLE
Jan Rillich, Birk Rillich, Paul A Stevenson
Aggression is a behavioral strategy for securing limited resources and its expression is strongly influenced by their presence and value. In particular, males are generally thought to guard females after mating to ward off other males, but the underlying control mechanisms are unknown. Here, we investigated the role of amines on male courtship behavior and its subsequent effect on male-male aggression in crickets (Gryllus bimaculatus). Contrary to the guarding hypothesis, female presence alone had no immediate effect on male-male aggression...
August 2019: Hormones and Behavior
https://read.qxmd.com/read/30457395/vortioxetine-a-novel-antidepressant-for-the-treatment-of-major-depressive-disorder
#16
REVIEW
Xenia Gonda, Samata R Sharma, Frank I Tarazi
Vortioxetine is a novel antidepressant drug approved for the treatment of major depressive disorder (MDD) in adults. It is formulated into tablets and has a dose range of 5-20 mg. The recommended starting dose is 10 mg administered orally once daily without the need for food. Areas covered: This review focuses on the preclinical and clinical discovery of vortioxetine. It analyzes the pharmacological, neurochemical, and behavioral mechanisms of the medication and how these contribute to its potential therapeutic advantages as described in published preclinical and clinical studies and product labels...
January 2019: Expert Opinion on Drug Discovery
https://read.qxmd.com/read/30382587/protein-kinase-c%C3%AE-constrains-the-s-pathway-to-phrenic-motor-facilitation-elicited-by-spinal-5-ht-7-receptors-or-severe-acute-intermittent-hypoxia
#17
JOURNAL ARTICLE
Raphael R Perim, Daryl P Fields, Gordon S Mitchell
KEY POINTS: Concurrent 5-HT2A (Q pathway) and 5-HT7 (S pathway) serotonin receptor activation cancels phrenic motor facilitation due to mutual cross-talk inhibition. Spinal protein kinase Cδ (PKCδ) or protein kinase A inhibition restores phrenic motor facilitation with concurrent Q and S pathway activation, demonstrating a key role for these kinases in cross-talk inhibition. Spinal PKCδ inhibition enhances adenosine-dependent severe acute intermittent hypoxia-induced phrenic long-term facilitation (S pathway), consistent with relief of cross-talk inhibition...
January 2019: Journal of Physiology
https://read.qxmd.com/read/30267130/the-5-ht-7-receptor-antagonist-sb-269970-ameliorates-corticosterone-induced-alterations-in-5-ht-7-receptor-mediated-modulation-of-gabaergic-transmission-in-the-rat-dorsal-raphe-nucleus
#18
JOURNAL ARTICLE
Joanna Sowa, Magdalena Kusek, Marcin Siwiec, Joanna Ewa Sowa, Bartosz Bobula, Krzysztof Tokarski, Grzegorz Hess
RATIONALE: Chronic stress and corticosterone have been shown to affect serotonin (5-HT) neurotransmission; however, the influence of stress on the activity of the dorsal raphe nucleus (DRN), the main source of 5-HT in the forebrain, is not well understood. In particular, it is unknown if and how stress modifies DRN 5-HT7 receptors, which are involved in the modulation of the firing of local inhibitory interneurons responsible for regulating the activity of DRN projection cells. OBJECTIVES: Our study aimed to investigate the effect of repeated corticosterone injections on the modulation of the inhibitory transmission within the DRN by 5-HT7 receptors and whether it could be reversed by treatment with a 5-HT7 receptor antagonist...
December 2018: Psychopharmacology
https://read.qxmd.com/read/30020772/pharmacology-and-therapeutic-potential-of-the-5-ht-7-receptor
#19
REVIEW
Kevin M Blattner, Daniel J Canney, Douglas A Pippin, Benjamin E Blass
It is well-documented that serotonin (5-HT) exerts its pharmacological effects through a series of 5-HT receptors. The most recently identified member of this family, 5-HT7 , was first identified in 1993. Over the course of the last 25 years, this receptor has been the subject of intense investigation, and it has been demonstrated that 5-HT7 plays an important role in a wide range of pharmacological processes. As a result of these findings, modulation of 5-HT7 activity has been the focus of numerous drug discovery and development programs...
January 16, 2019: ACS Chemical Neuroscience
https://read.qxmd.com/read/29384698/cross-talk-inhibition-between-5-ht-2b-and-5-ht-7-receptors-in-phrenic-motor-facilitation-via-nadph-oxidase-and-pka
#20
JOURNAL ARTICLE
Raphael R Perim, Daryl P Fields, Gordon S Mitchell
Intermittent spinal serotonin receptor activation elicits phrenic motor facilitation (pMF), a form of spinal respiratory motor plasticity. Episodic activation of either serotonin type 2 (5-HT2 ) or type 7 (5-HT7 ) receptors elicits pMF, although they do so via distinct cellular mechanisms known as the Q (5-HT2 ) and S (5-HT7 ) pathways to pMF. When coactivated, these pathways interact via mutual cross-talk inhibition. Although we have a rudimentary understanding of mechanisms mediating cross-talk interactions between spinal 5-HT2 subtype A (5-HT2A ) and 5-HT7 receptor activation, we do not know if similar interactions exist between 5-HT2 subtype B (5-HT2B ) and 5-HT7 receptors...
May 1, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
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