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Schizophrenia histamine

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https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#1
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/28614417/antipsychotic-medications-and-stroke-in-schizophrenia-a-case-crossover-study
#2
Wen-Yin Chen, Lian-Yu Chen, Hsing-Cheng Liu, Chi-Shin Wu, Shu-Yu Yang, Chun-Hung Pan, Shang-Ying Tsai, Chiao-Chicy Chen, Chian-Jue Kuo
BACKGROUND: The association between antipsychotic use and the risk of stroke in schizophrenic patients is controversial. We sought to study the association in a nationwide cohort with schizophrenia. METHODS: Using a retrospective cohort of patients with schizophrenia (N = 31,976) derived from the Taiwan National Health Insurance Research Database, 802 new-onset cases of stroke were identified within 10 years of follow-up (from 2000 through 2010). We designed a case-crossover study using 14-day windows to explore the risk factors of stroke and the association between antipsychotic drugs and the risk of stroke...
2017: PloS One
https://www.readbyqxmd.com/read/28557969/-metabolic-safety-of-antidepressant-medicines
#3
Wojciech Łężak, Łukasz Mokros, Michał Seweryn Karbownik, Andrzej Witusik, Marcin Kosmalski, Edward Kowalczyk, Tadeusz Pietras
Metabolic syndrome is a very serious health issue, not only from internal medicine's point of view. Patients suffering from overweight, arterial hypertension, lipids and carbohydrates metabolism disorders are also in the circle of interest of other areas of medicine, including psychiatry. Currently, one of key problems of pharmacotherapy is a comorbidity of metabolic syndrome and mental disorder. Depression is more common than schizophrenia. Despite the fact that in everyday clinical practice there are more patients with depression than schizophrenia, there is a bigger interest among scientists for metabolic syndrome after antipsychotic drugs than as an effect of use of antidepressant agents...
May 23, 2017: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/28463343/biological-treatment-of-acute-agitation-or-aggression-with-schizophrenia-or-bipolar-disorder-in-the-inpatient-setting
#4
Christoph U Correll, Xin Yu, Yutao Xiang, John M Kane, Prakash Masand
BACKGROUND: Schizophrenia and bipolar disorders are chronic illnesses that commonly present with symptoms of acute agitation and aggression. These symptoms must be managed rapidly to prevent potential harm to the patient and others, including their caregivers, peers, and health care workers. A number of treatment options are available to clinicians to manage acute agitation and aggression, including non-pharmacologic behavioral and environmental de-escalation strategies, as well as biological treatment options such as pharmacologic agents and electroconvulsive therapy...
May 2017: Annals of Clinical Psychiatry: Official Journal of the American Academy of Clinical Psychiatrists
https://www.readbyqxmd.com/read/28400155/histaminergic-gene-polymorphisms-associated-with-sedation-in-clozapine-treated-patients
#5
Anssi Solismaa, Olli Kampman, Leo-Pekka Lyytikäinen, Niko Seppälä, Merja Viikki, Nina Mononen, Terho Lehtimäki, Esa Leinonen
Sedation is a common adverse effect of clozapine treatment, which may be partly related to clozapine binding to histamine receptors in the central nervous system. The objective of this study was to investigate whether single nucleotide polymorphisms (SNPs) in the histaminergic system are associated with sedation in clozapine-treated patients. The study population comprised 237 clozapine-treated, Finnish, Caucasian patients that were diagnosed with schizophrenia and 176 were genotyped using Illumina HumanCoreExome-12 BeadChip...
April 8, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28274820/histamine-induces-kcnq-channel-dependent-gamma-oscillations-in-rat-hippocampus-via-activation-of-the-h1-receptor
#6
Richard Andersson, Dagmar Galter, Daniela Papadia, André Fisahn
Histamine is an aminergic neurotransmitter, which regulates wakefulness, arousal and attention in the central nervous system. Histamine receptors have been the target of efforts to develop pro-cognitive drugs to treat disorders such as Alzheimer's disease and schizophrenia. Cognitive functions including attention are closely associated with gamma oscillations, a rhythmical electrical activity pattern in the 30-80 Hz range, which depends on the synchronized activity of excitatory pyramidal cells and inhibitory fast-spiking interneurons...
May 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28223162/the-roles-of-histamine-and-its-receptor-ligands-in-central-nervous-system-disorders-an-update
#7
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/27855565/impact-of-histamine-receptors-h1-and-h3-polymorphisms-on-antipsychotic-induced-weight-gain
#8
Arun K Tiwari, Danning Zhang, Jennie G Pouget, Clement C Zai, Nabilah I Chowdhury, Eva J Brandl, Li Qin, Natalie Freeman, Jeffrey A Lieberman, Herbert Y Meltzer, James L Kennedy, Daniel J Müller
OBJECTIVES: A positive correlation between antipsychotic-induced weight gain (AIWG) and the antagonist effect of antipsychotic drugs at the histamine H1 receptor (HRH1) as well as the agonist effect at the histamine H3 receptor (HRH3) in the brain has been consistently demonstrated. We investigated the potential impact of single-nucleotide polymorphisms (SNPs) in HRH1 and HRH3 genes on AIWG. METHODS: We analysed 40 tagSNPs in HRH1 (n = 34) and HRH3 (n = 6) in schizophrenia/schizoaffective disorder patients (n = 193) primarily treated with clozapine or olanzapine for up to 14 weeks...
December 15, 2016: World Journal of Biological Psychiatry
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#9
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27502027/discriminative-stimulus-properties-of-1-25mg-kg-clozapine-in-rats-mediation-by-serotonin-5-ht2-and-dopamine-d4-receptors
#10
Adam J Prus, Laura E Wise, Alan L Pehrson, Scott D Philibin, Benny Bang-Andersen, Jørn Arnt, Joseph H Porter
The atypical antipsychotic drug clozapine remains one of most effective treatments for schizophrenia, given a lack of extrapyramidal side effects, improvements in negative symptoms, cognitive impairment, and in symptoms in treatment-resistant schizophrenia. The adverse effects of clozapine, including agranulocytosis, make finding a safe clozapine-like a drug a goal for drug developers. The drug discrimination paradigm is a model of interoceptive stimulus that has been used in an effort to screen experimental drugs for clozapine-like atypical antipsychotic effects...
October 1, 2016: Brain Research
https://www.readbyqxmd.com/read/27372312/antipsychotic-drug-induced-somnolence-incidence-mechanisms-and-management
#11
REVIEW
Fang Fang, Hongwei Sun, Zuowei Wang, Ming Ren, Joseph R Calabrese, Keming Gao
Somnolence is a common side effect of antipsychotics. To assess the incidence of this side effect, we performed a MEDLINE search for randomized, double-blinded, placebo- or active-controlled studies of adult patients treated with antipsychotics for schizophrenia, mania, bipolar depression, or bipolar disorder. We extracted rates of somnolence from original publications and pooled them based on the dose of each antipsychotic in the same psychiatric condition, then estimated the absolute risk increase (ARI) and the number needed to harm (NNH) of an antipsychotic relative to placebo or an active comparator in the same psychiatric condition...
September 2016: CNS Drugs
https://www.readbyqxmd.com/read/27368152/involvement-of-the-histamine-h4-receptor-in-clozapine-induced-hematopoietic-toxicity-vulnerability-under-granulocytic-differentiation-of-hl-60-cells
#12
Aya Goto, Akihiro Mouri, Tomoko Nagai, Akira Yoshimi, Mako Ukigai, Tomomi Tsubai, Hirotake Hida, Norio Ozaki, Yukihiro Noda
Clozapine is an effective antipsychotic for treatment-resistant schizophrenia, but can cause fatal hematopoietic toxicity as agranulocytosis. To elucidate the mechanism of hematopoietic toxicity induced by clozapine, we developed an in vitro assay system using HL-60 cells, and investigated the effect on hematopoiesis. HL-60 cells were differentiated by all-trans retinoic acid (ATRA) into three states according to the following hematopoietic process: undifferentiated HL-60 cells, those undergoing granulocytic ATRA-differentiation, and ATRA-differentiated granulocytic cells...
September 1, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/27363923/histamine-h3-receptor-as-a-potential-target-for-cognitive-symptoms-in-neuropsychiatric-diseases
#13
REVIEW
Bassem Sadek, Ali Saad, Adel Sadeq, Fakhreya Jalal, Holger Stark
The potential contributions of the brain histaminergic system in neurodegenerative diseases, and the possiblity of histamine-targeting treatments is attracting considerable interests. The histamine H3 receptor (H3R) is expressed mainly in the central nervous system, and is, consequently, an attractive pharmacological target. Although recently described clinical trials have been disappointing in attention deficit hyperactivity disorder (ADHD) and schizophrenia (SCH), numerous H3R antagonists, including pitolisant, demonstrate potential in the treatment of narcolepsy, excessive daytime sleepiness associated with cognitive impairment, epilepsy, and Alzheimer's disease (AD)...
October 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27232215/avn-101-a-multi-target-drug-candidate-for-the-treatment-of-cns-disorders
#14
Alexandre V Ivachtchenko, Yan Lavrovsky, Ilya Okun
Lack of efficacy of many new highly selective and specific drug candidates in treating diseases with poorly understood or complex etiology, as are many of central nervous system (CNS) diseases, encouraged an idea of developing multi-modal (multi-targeted) drugs. In this manuscript, we describe molecular pharmacology, in vitro ADME, pharmacokinetics in animals and humans (part of the Phase I clinical studies), bio-distribution, bioavailability, in vivo efficacy, and safety profile of the multimodal drug candidate, AVN-101...
May 25, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27092339/cariprazine-new-dopamine-biased-agonist-for-neuropsychiatric-disorders
#15
REVIEW
P De Deurwaerdère
Cariprazine (RGH-188, MP-214, Vraylar[TM]) is a new dopamine receptor ligand developed for the treatment of several neuropsychiatric diseases including schizophrenia and bipolar disorders. Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors. At variance with some atypical antipsychotics, its affinity at 5-HT1A, 5-HT2A and histamine H1 receptors is modest compared with its three main targets. Cariprazine could correspond to a biased agonist at dopamine receptors, displaying either antagonist or partial agonist properties depending on the signaling pathways linked to D2/D3 receptors...
February 2016: Drugs of Today
https://www.readbyqxmd.com/read/27092049/trace-amines-and-the-trace-amine-associated-receptor-1-pharmacology-neurochemistry-and-clinical-implications
#16
REVIEW
Yue Pei, Aman Asif-Malik, Juan J Canales
Biogenic amines are a collection of endogenous molecules that play pivotal roles as neurotransmitters and hormones. In addition to the "classical" biogenic amines resulting from decarboxylation of aromatic acids, including dopamine (DA), norepinephrine, epinephrine, serotonin (5-HT), and histamine, other biogenic amines, present at much lower concentrations in the central nervous system (CNS), and hence referred to as "trace" amines (TAs), are now recognized to play significant neurophysiological and behavioral functions...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27089413/histamine-h3-receptor-antagonists-display-antischizophrenic-activities-in-rats-treated-with-mk-801
#17
Danish Mahmood, Mohd Akhtar, Kausar Jahan, Dipanjan Goswami
BACKGROUND: Animal models based on N-methyl-d-aspartate receptor blockade have been extensively used for schizophrenia. Ketamine and MK-801 produce behaviors related to schizophrenia and exacerbated symptoms in patients with schizophrenia, which led to the use of PCP (phencyclidine)- and MK-801 (dizocilpine)-treated animals as models for schizophrenia. METHODS: The study investigated the effect of subchronic dosing (once daily, 7 days) of histamine H3 receptor (H3R) antagonists, ciproxifan (CPX) (3 mg/kg, i...
September 1, 2016: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/27028981/a-randomized-double-blind-placebo-controlled-pilot-study-of-betahistine-to-counteract-olanzapine-associated-weight-gain
#18
RANDOMIZED CONTROLLED TRIAL
Nir Barak, Yaffa Beck, Joseph H Albeck
Patients with schizophrenia experience higher rates of obesity and related morbidity and mortality than the general population does. Given preclinical studies revealing the role of histamine H1 receptor in human eating behavior, and the potential of olanzapine to block with this system, we hypothesized that histamine H1 receptor agonists may be beneficial in reducing antipsychotic-associated weight gain. In the present study, 36 patients with a diagnosis of schizophrenia or schizoaffective disorder and treated with olanzapine were randomized to betahistine (48 mg/d) or matching placebo for 16 weeks...
June 2016: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/26839321/betahistine-decreases-olanzapine-induced-weight-gain-and-somnolence-in-humans
#19
RANDOMIZED CONTROLLED TRIAL
Nir Barak, Yaffa Beck, Joseph H Albeck
Olanzapine's efficacy in schizophrenia is attributed to antagonism of dopamine and serotonin receptors. Olanzapine is also a potent histamine-H1 antagonist that results in weight gain and somnolence. Betahistine is a centrally acting histamine-H1 agonist, and therefore may reduce olanzapine's effect on histamine receptors in the brain. Olanzapine's high affinity for the histamine-H1 receptor warrants the use of high doses of betahistine. Forty-eight healthy women were recruited and randomized to receive either betahistine 144 mg/day or matching placebo for 4 weeks...
March 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/26446869/effects-of-nmda-receptor-antagonists-and-antipsychotics-on-high-frequency-oscillations-recorded-in-the-nucleus-accumbens-of-freely-moving-mice
#20
Mark J Hunt, Maciej Olszewski, Joanna Piasecka, Miles A Whittington, Stefan Kasicki
RATIONALE: Abnormal oscillatory activity associated with N-methyl-D-aspartate (NMDA) receptor hypofunction is widely considered to contribute to the symptoms of schizophrenia. OBJECTIVE: This study aims to characterise the changes produced by NMDA receptor antagonists and antipsychotics on accumbal high-frequency oscillations (HFO; 130-180 Hz) in mice. METHODS: Local field potentials were recorded from the nucleus accumbens of freely moving mice...
December 2015: Psychopharmacology
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