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Parkinson histamine

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https://www.readbyqxmd.com/read/29191006/selective-and-mechanically-robust-sensors-for-electrochemical-measurements-of-real-time-hydrogen-peroxide-dynamics-in-vivo
#1
Leslie R Wilson, Sambit Panda, Andreas C Schmidt, Leslie A Sombers
The role of hydrogen peroxide (H2O2) in the complex environment of the brain is not well understood. H2O2 plays several important roles - for instance, it serves as a key chemical player in normal physiological processes such as cellular respiration, a modulator of dopaminergic signaling, and its presence can indicate the upstream production of more aggressive and short-lived reactive oxygen species (ROS). As such, H2O2 has been implicated in several neurodegenerative diseases, including the slow destruction of dopaminergic neurons in Parkinson's disease (PD)...
December 1, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29184503/pharmacological-characterization-of-5-substituted-1-2-3-dihydro-1-benzofuran-2-yl-methyl-piperazines-novel-antagonists-for-the-histamine-h3-and-h4-receptors-with-anti-inflammatory-potential
#2
Michelle F Corrêa, Álefe J R Barbosa, Larissa B Teixeira, Diego A Duarte, Sarah C Simões, Lucas T Parreiras-E-Silva, Aleksandro M Balbino, Richardt G Landgraf, Michel Bouvier, Claudio M Costa-Neto, João P S Fernandes
The histamine receptors (HRs) are traditional G protein-coupled receptors of extensive therapeutic interest. Recently, H3R and H4R subtypes have been targeted in drug discovery projects for inflammation, asthma, pain, cancer, Parkinson's, and Alzheimer's diseases, which includes searches for dual acting H3R/H4R ligands. In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazine (LINS01 series) molecules were synthesized and evaluated as H3R and H4R ligands. Our data show that the N-allyl-substituted compound LINS01004 bears the highest affinity for H3R (pKi 6...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29102759/preclinical-profile-of-a-dopamine-d1-potentiator-suggests-therapeutic-utility-in-neurological-and-psychiatric-disorders
#3
Robert F Bruns, Stephen N Mitchell, Keith A Wafford, Alex J Harper, Elaine A Shanks, Guy Carter, Michael J O'Neill, Tracey K Murray, Brian J Eastwood, John M Schaus, James P Beck, Junliang Hao, Jeffrey M Witkin, Xia Li, Eyassu Chernet, Jason S Katner, Hong Wang, John W Ryder, Meghane E Masquelin, Linda K Thompson, Patrick L Love, Deanna L Maren, Julie F Falcone, Michelle M Menezes, Linli Zhang, Charles R Yang, Kjell A Svensson
DETQ, an allosteric potentiator of the dopamine D1 receptor, was tested in therapeutic models that were known to respond to D1 agonists. Because of a species difference in affinity for DETQ, all rodent experiments used transgenic mice expressing the human D1 receptor (hD1 mice). When given alone, DETQ reversed the locomotor depression caused by a low dose of reserpine. DETQ also acted synergistically with L-DOPA to reverse the strong hypokinesia seen with a higher dose of reserpine. These results indicate potential as both monotherapy and adjunct treatment in Parkinson's disease...
January 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29061777/possible-biological-and-clinical-applications-of-phenothiazines
#4
REVIEW
Borisz Varga, Ákos Csonka, Andrea Csonka, Joseph Molnár, Leonard Amaral, Gabriella Spengler
Phenothiazines have been used in many areas of medicine, mainly in psychopharmacology. These compounds are able to effectively inhibit dopamine, histamine, serotonin, acetylcholine, and α-adrenergic receptors; thus, their effect and side-effect profiles are extremely diverse. Besides their antipsychotic activity, phenothiazines have a significant antimicrobial effect as well, since they can enhance the bactericidal function of macrophages and inhibit efflux pumps. They are also able to eliminate bacterial resistance plasmids and destroy bacteria by their membrane-destabilizing effect...
November 2017: Anticancer Research
https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#5
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28748860/current-nondopaminergic-therapeutic-options-for-motor-symptoms-of-parkinson-s-disease
#6
REVIEW
Juan-Juan Du, Sheng-Di Chen
OBJECTIVE: The aim of this study was to summarize recent studies on nondopaminergic options for the treatment of motor symptoms in Parkinson's disease (PD). DATA SOURCES: Papers in English published in PubMed, Cochrane, and Ovid Nursing databases between January 1988 and November 2016 were searched using the following keywords: PD, nondopaminergic therapy, adenosine, glutamatergic, adrenergic, serotoninergic, histaminic, and iron chelator. We also reviewed the ongoing clinical trials in the website of clinicaltrials...
August 5, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28698624/naringenin-impairs-two-pore-channel-2-activity-and-inhibits-vegf-induced-angiogenesis
#7
Irene Pafumi, Margherita Festa, Francesca Papacci, Laura Lagostena, Cristina Giunta, Vijay Gutla, Laura Cornara, Annarita Favia, Fioretta Palombi, Franco Gambale, Antonio Filippini, Armando Carpaneto
Our research introduces the natural flavonoid naringenin as a novel inhibitor of an emerging class of intracellular channels, Two-Pore Channel 2 (TPC2), as shown by electrophysiological evidence in a heterologous system, i.e. Arabidopsis vacuoles lacking endogenous TPCs. In view of the control exerted by TPC2 on intracellular calcium signaling, we demonstrated that naringenin dampens intracellular calcium responses of human endothelial cells stimulated with VEGF, histamine or NAADP-AM, but not with ATP or Angiopoietin-1 (negative controls)...
July 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28520722/altered-detrusor-contractility-in-mptp-treated-common-marmosets-with-bladder-hyperreflexia
#8
Sara Pritchard, Michael J Jackson, Atsuko Hikima, Lisa Lione, Christopher D Benham, K Ray Chaudhuri, Sarah Rose, Peter Jenner, Mahmoud M Iravani
Bladder hyperreflexia is a common non-motor feature of Parkinson's disease. We now report on the contractility of the isolated primate detrusor strips devoid of nerve input and show that following MPTP, the amplitude and frequency of spontaneous contraction was increased. These responses were unaffected by dopamine D1 and D2 receptor agonists A77636 and ropinirole respectively. Contractions by exogenous carbachol, histamine or ATP were similar and no differences in the magnitude of noradrenaline-induced relaxation were seen in detrusor strip obtained from normal and MPTP-treated common marmosets (Callithrix jacchus)...
2017: PloS One
https://www.readbyqxmd.com/read/28398338/the-histamine-h3-receptor-antagonist-thioperamide-rescues-circadian-rhythm-and-memory-function-in-experimental-parkinsonism
#9
D Masini, C Lopes-Aguiar, A Bonito-Oliva, D Papadia, R Andersson, A Fisahn, G Fisone
Parkinson's disease (PD) is a common neurodegenerative disorder, characterized by motor impairment and a wide range of non-motor symptoms, including sleep disorders and cognitive and affective deficits. In this study, we used a mouse model of PD based on 6-hydroxydopamine (6-OHDA) to examine the effect of thioperamide, a histamine H3 receptor antagonist, on circadian activity, recognition memory and anxiety. A partial, bilateral 6-OHDA lesion of the striatum reduces motor activity during the active phase of the 24 h cycle...
April 11, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28223162/the-roles-of-histamine-and-its-receptor-ligands-in-central-nervous-system-disorders-an-update
#10
REVIEW
Weiwei Hu, Zhong Chen
The neurotransmitter histamine receives less attention compared with other biogenic amines, because of its moderate action in the central nervous system (CNS). However, recent evidence suggests that histamine plays an important role in multiple CNS disorders including insomnia, narcolepsy, Parkinson's diseases, schizophrenia, Alzheimer's disease, and cerebral ischemia. New insights are emerging into the potential roles of histamine receptors as targets for the treatment of these diseases. Although some histamine related agents have failed in clinical trials, current preclinical studies suggest that this neurotransmitter may still have extensive applications in treating CNS disorders, however, advanced studies are warranted...
February 20, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28052533/what-a-difference-a-methyl-group-makes-the-selectivity-of-monoamine-oxidase%C3%A2-b-towards-histamine-and-n-methylhistamine
#11
Aleksandra Maršavelski, Robert Vianello
Monoamine oxidase (MAO) enzymes catalyze the degradation of a very broad range of biogenic and dietary amines including many neurotransmitters in the brain, whose imbalance is extensively linked with the biochemical pathology of various neurological disorders. Although sharing around 70 % sequence identity, both MAO A and B isoforms differ in substrate affinities and inhibitor sensitivities. Inhibitors that act on MAO A are used to treat depression, due to their ability to raise serotonin concentrations, whereas MAO B inhibitors decrease dopamine degradation and improve motor control in patients with Parkinson disease...
February 24, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27881066/new-insights-emerging-from-recent-investigations-on-human-group-ii-pyridoxal-5-phosphate-decarboxylases
#12
REVIEW
Alessandro Paiardini, Giorgio Giardina, Giada Rossignoli, Carla Borri Voltattorni, Mariarita Bertoldi
Aromatic amino acid, cysteine sulfinic acid, glutamate and histidine decarboxylases, belonging to group II of pyridoxal 5'-phosphate-dependent enzymes, catalyze the synthesis of dopamine/serotonin, hypotaurine, γ-aminobutyric acid and histamine, respectively. Considering that these reaction products are all essential bioactive molecules, group II decarboxylases have been long studied from an evolutionary, biochemical and pharmacological standpoint. Despite the fact that they all belong to a common fold-type, during evolution each decarboxylase has evolved unique structural elements responsible for its substrate specificity...
2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27837280/thr105ile-rs11558538-polymorphism-in-the-histamine-1-methyl-transferase-hnmt-gene-and-risk-for-restless-legs-syndrome
#13
Félix Javier Jiménez-Jiménez, Elena García-Martín, Hortensia Alonso-Navarro, Carmen Martínez, Martín Zurdo, Laura Turpín-Fenoll, Jorge Millán-Pascual, Teresa Adeva-Bartolomé, Esther Cubo, Francisco Navacerrada, Ana Rojo-Sebastián, Lluisa Rubio, Sara Ortega-Cubero, Pau Pastor, Marisol Calleja, José Francisco Plaza-Nieto, Belén Pilo-de-la-Fuente, Margarita Arroyo-Solera, Esteban García-Albea, José A G Agúndez
A recent meta-analysis suggests an association between the rs11558538 single nucleotide polymorphism in the histamine-N-methyl-transferase (HNMT) gene and the risk for Parkinson's disease. Based on the possible relationship between PD and restless legs syndrome (RLS), we tried to establish whether rs11558538 SNP is associated with the risk for RLS. We studied the genotype and allelic variant frequencies of HNMT rs11558538 SNP 205 RLS patients and 410 healthy controls using a TaqMan assay. The frequencies of the HNMT rs11558538 genotypes allelic variants were similar between RLS patients and controls, and were not influenced by gender, family history of RLS, or RLS severity...
March 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/27836486/immunochemical-localization-of-vesicular-monoamine-transporter-2-vmat2-in-mouse-brain
#14
Rachel A Cliburn, Amy R Dunn, Kristen A Stout, Carlie A Hoffman, Kelly M Lohr, Alison I Bernstein, Emily J Winokur, James Burkett, Yvonne Schmitz, William M Caudle, Gary W Miller
Vesicular monoamine transporter 2 (VMAT2, SLC18A2) is a transmembrane transporter protein that packages dopamine, serotonin, norepinephrine, and histamine into vesicles in preparation for neurotransmitter release from the presynaptic neuron. VMAT2 function and related vesicle dynamics have been linked to susceptibility to oxidative stress, exogenous toxicants, and Parkinson's disease. To address a recent depletion of commonly used antibodies to VMAT2, we generated and characterized a novel rabbit polyclonal antibody generated against a 19 amino acid epitope corresponding to an antigenic sequence within the C-terminal tail of mouse VMAT2...
October 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/27563055/the-histamine-h3-receptor-structure-pharmacology-and-function
#15
REVIEW
Gustavo Nieto-Alamilla, Ricardo Márquez-Gómez, Ana-Maricela García-Gálvez, Guadalupe-Elide Morales-Figueroa, José-Antonio Arias-Montaño
Among the four G protein-coupled receptors (H1-H4) identified as mediators of the biologic effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive expression in the nervous system and the large variety of isoforms generated by alternative splicing of the corresponding mRNA. Additionally, it exhibits dual functionality as autoreceptor and heteroreceptor, and this enables H3Rs to modulate the histaminergic and other neurotransmitter systems. The cloning of the H3R cDNA in 1999 by Lovenberg et al...
November 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27539857/a-novel-developmental-role-for-dopaminergic-signaling-to-specify-hypothalamic-neurotransmitter-identity
#16
Yu-Chia Chen, Svetlana Semenova, Stanislav Rozov, Maria Sundvik, Joshua L Bonkowsky, Pertti Panula
Hypothalamic neurons expressing histamine and orexin/hypocretin (hcrt) are necessary for normal regulation of wakefulness. In Parkinson's disease, the loss of dopaminergic neurons is associated with elevated histamine levels and disrupted sleep/wake cycles, but the mechanism is not understood. To characterize the role of dopamine in the development of histamine neurons, we inhibited the translation of the two non-allelic forms of tyrosine hydroxylase (th1 and th2) in zebrafish larvae. We found that dopamine levels were reduced in both th1 and th2 knockdown, but the serotonin level and number of serotonin neurons remained unchanged...
October 14, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27399132/thr105ile-rs11558538-polymorphism-in-the-histamine-n-methyltransferase-hnmt-gene-and-risk-for-parkinson-disease-a-prisma-compliant-systematic-review-and-meta-analysis
#17
REVIEW
Félix Javier Jiménez-Jiménez, Hortensia Alonso-Navarro, Elena García-Martín, José A G Agúndez
BACKGROUND/AIMS: Several neuropathological, biochemical, and pharmacological data suggested a possible role of histamine in the etiopathogenesis of Parkinson disease (PD). The single nucleotide polymorphism (SNP) rs11558538 in the histamine N-methyltransferase (HNMT) gene has been associated with the risk of developing PD by several studies but not by some others. We carried out a systematic review that included all the studies published on PD risk related to the rs11558538 SNP, and we conducted a meta-analysis following Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines...
July 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27260166/histamine-induces-microglia-activation-and-dopaminergic-neuronal-toxicity-via-h1-receptor-activation
#18
Sandra M Rocha, Tatiana Saraiva, Ana C Cristóvão, Raquel Ferreira, Tiago Santos, Marta Esteves, Cláudia Saraiva, Goun Je, Luísa Cortes, Jorge Valero, Gilberto Alves, Alexander Klibanov, Yoon-Seong Kim, Liliana Bernardino
BACKGROUND: Histamine is an amine widely known as a peripheral inflammatory mediator and as a neurotransmitter in the central nervous system. Recently, it has been suggested that histamine acts as an innate modulator of microglial activity. Herein, we aimed to disclose the role of histamine in microglial phagocytic activity and reactive oxygen species (ROS) production and to explore the consequences of histamine-induced neuroinflammation in dopaminergic (DA) neuronal survival. METHODS: The effect of histamine on phagocytosis was assessed both in vitro by using a murine N9 microglial cell line and primary microglial cell cultures and in vivo...
June 4, 2016: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/27190492/histamine-and-immune-biomarkers-in-cns-disorders
#19
REVIEW
Ramón Cacabelos, Clara Torrellas, Lucía Fernández-Novoa, Francisco López-Muñoz
Neuroimmune dysregulation is a common phenomenon in different forms of central nervous system (CNS) disorders. Cross-links between central and peripheral immune mechanisms appear to be disrupted as reflected by a series of immune markers (CD3, CD4, CD7, HLA-DR, CD25, CD28, and CD56) which show variability in brain disorders such as anxiety, depression, psychosis, stroke, Alzheimer's disease, Parkinson's disease, attention-deficit hyperactivity disorder, migraine, epilepsy, vascular dementia, mental retardation, cerebrovascular encephalopathy, multiple sclerosis, brain tumors, cranial nerve neuropathies, mental retardation, and posttraumatic brain injury...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27145922/meclizine-induced-enhanced-glycolysis-is-neuroprotective-in-parkinson-disease-cell-models
#20
Chien Tai Hong, Kai-Yin Chau, Anthony H V Schapira
Meclizine is a well-tolerated drug routinely used as an anti-histamine agent in the management of disequilibrium. Recently, meclizine has been assessed for its neuroprotective properties in ischemic stroke and Huntington disease models. We found that meclizine protected against 6-hydroxydopamine-induced apoptosis and cell death in both SH-SY5Y cells and rat primary cortical cultures. Meclizine increases the level of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which activates phosphofructokinase, a rate-determining enzyme of glycolysis...
May 5, 2016: Scientific Reports
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