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D2 receptor weight gain

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https://www.readbyqxmd.com/read/28602634/dp1-receptor-agonist-bw245c-inhibits-diet-induced-obesity-in-apoe-mice
#1
Sunil Kumar, Thomas Palaia, Christopher Hall, Louis Ragolia
BACKGROUND/OBJECTIVE: Lipocalin Prostaglandin D2 synthase (LPGDS) contributes to the production of PGD2, which has been associated with adipogenesis. In this study, we aimed to investigate the role of PGD2 on obesity through its DP1 and DP2 receptor signaling using intraperitoneal injection of their respective agonists and antagonists. METHODS: ApoE(-/-) mice were divided into five groups: vehicle control (n=5), DP1 receptor agonist (n=5), DP1 receptor antagonist (n=5), DP2 receptor agonist (n=5), and DP2 receptor antagonist (n=5), and the study was carried out for 10 weeks...
June 8, 2017: Obesity Research & Clinical Practice
https://www.readbyqxmd.com/read/28560263/dopamine-d2-receptors-and-the-circadian-clock-reciprocally-mediate-antipsychotic-drug-induced-metabolic-disturbances
#2
Zachary Freyberg, Michael J McCarthy
Antipsychotic drugs are widely prescribed medications, used for numerous psychiatric illnesses. However, antipsychotic drugs cause serious metabolic side effects that can lead to substantial weight gain and increased risk for type 2 diabetes. While individual drugs differ, all antipsychotic drugs may cause these important side effects to varying degrees. Given that the single unifying property shared by these medications is blockade of dopamine D2 and D3 receptors, these receptors likely play a role in antipsychotic drug-induced metabolic side effects...
2017: NPJ Schizophrenia
https://www.readbyqxmd.com/read/28521704/dopamine-d2-receptors-dimers-how-can-we-pharmacologically-target-them
#3
Marco Carli, Shivakumar Kolachalam, Stefano Aringhieri, Mario Rossi, Luca Giovannini, Roberto Maggio, Marco Scarselli
Dopamine D2 and D3 receptors are important pharmacological targets in Schizophrenia and Parkinson’s disease. Intriguingly, many studies have shown that they form homo- and heterodimers, and they can be targeted in specific tissues with new drugs. In this direction, many efforts have been made to develop new molecules that are able to interact with these receptor dimeric complexes. Among various strategies for targeting dopamine receptors dimers, two distinct classes of compounds, such as bivalent and bitopic ligands, have gained particular attention and their use in pharmacology looks promising...
May 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28478771/evaluation-of-the-long-term-safety-and-tolerability-of-cariprazine-in-patients-with-schizophrenia-results-from-a-1-year-open-label-study
#4
Andrew J Cutler, Suresh Durgam, Yao Wang, Raffaele Migliore, Kaifeng Lu, István Laszlovszky, György Németh
OBJECTIVE: Cariprazine, a dopamine D3/D2 partial agonist atypical antipsychotic with preferential binding to D3 receptors, is approved for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder. The efficacy and safety of cariprazine was established in three randomized, double-blind, placebo-controlled, 6-week trials in patients with acute exacerbation of schizophrenia. This 53-week study evaluated the long-term safety and tolerability of cariprazine in patients with schizophrenia...
May 8, 2017: CNS Spectrums
https://www.readbyqxmd.com/read/28368577/classics-in-chemical-neuroscience-aripiprazole
#5
Austen B Casey, Clinton E Canal
Aripiprazole was the first antipsychotic developed to possess agonist properties at dopamine D2 autoreceptors, a groundbreaking strategy that presented a new vista for schizophrenia drug discovery. The dopamine D2 receptor is the crucial target of all extant antipsychotics, and all developed prior to aripiprazole were D2 receptor antagonists. Extensive blockade of these receptors, however, typically produces extrapyramidal (movement) side effects, which plagued first-generation antipsychotics, such as haloperidol...
June 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28334444/the-partial-dopamine-d2-receptor-agonist-aripiprazole-is-associated-with-weight-gain-in-adolescent-anorexia-nervosa
#6
Guido K W Frank, Megan E Shott, Jennifer O Hagman, Marissa A Schiel, Marisa C DeGuzman, Brogan Rossi
OBJECTIVE: Finding medication to support treatment of anorexia nervosa has been difficult. Neuroscience-based approaches may help in this effort. Recent brain imaging studies in adults and adolescents with anorexia nervosa suggest that dopamine-related reward circuits are hypersensitive and could provide a treatment target. METHODS: Here, we present a retrospective chart review of 106 adolescents with anorexia nervosa some of whom were treated with the dopamine D2 receptor partial agonist aripiprazole during treatment in a specialized eating disorder program...
April 2017: International Journal of Eating Disorders
https://www.readbyqxmd.com/read/28331332/clinical-role-of-brexpiprazole-in-depression-and-schizophrenia
#7
REVIEW
Nishant B Parikh, Diana M Robinson, Anita H Clayton
Brexpiprazole, a serotonin-dopamine activity modulator, is the second D2 partial agonist to come to market and has been approved for the treatment of schizophrenia and as an adjunctive treatment in major depressive disorder. With less intrinsic activity than aripiprazole at the D2 receptor and higher potency at 5-HT2A, 5-HT1A, and α1B receptors, the pharmacological properties of brexpiprazole suggest a more tolerable side effect profile with regard to akathisia, extrapyramidal dysfunction, and sedation. While no head-to-head data are currently available, double-blind placebo-controlled studies show favorable results, with the number needed to treat (NNT) vs placebo of 6-15 for response in acute schizophrenia treatment and 4 for maintenance...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28041956/basal-ganglia-dysfunction-contributes-to-physical-inactivity-in-obesity
#8
Danielle M Friend, Kavya Devarakonda, Timothy J O'Neal, Miguel Skirzewski, Ioannis Papazoglou, Alanna R Kaplan, Jeih-San Liow, Juen Guo, Sushil G Rane, Marcelo Rubinstein, Veronica A Alvarez, Kevin D Hall, Alexxai V Kravitz
Obesity is associated with physical inactivity, which exacerbates the health consequences of weight gain. However, the mechanisms that mediate this association are unknown. We hypothesized that deficits in dopamine signaling contribute to physical inactivity in obesity. To investigate this, we quantified multiple aspects of dopamine signaling in lean and obese mice. We found that D2-type receptor (D2R) binding in the striatum, but not D1-type receptor binding or dopamine levels, was reduced in obese mice. Genetically removing D2Rs from striatal medium spiny neurons was sufficient to reduce motor activity in lean mice, whereas restoring Gi signaling in these neurons increased activity in obese mice...
February 7, 2017: Cell Metabolism
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/27440212/cariprazine-for-the-treatment-of-schizophrenia-a-review-of-this-dopamine-d3-preferring-d3-d2-receptor-partial-agonist
#10
REVIEW
Leslie Citrome
Cariprazine is an antipsychotic medication and received approval by the U.S. Food and Drug Administration for the treatment of schizophrenia in September 2015. Cariprazine is a dopamine D3 and D2 receptor partial agonist, with a preference for the D3 receptor. Cariprazine is also a partial agonist at the serotonin 5-HT1A receptor and acts as an antagonist at 5-HT2B and 5-HT2A receptors. The recommended dose range of cariprazine for the treatment of schizophrenia is 1.5-6 mg/d; the starting dose of 1.5 mg/d is potentially therapeutic...
2016: Clinical Schizophrenia & related Psychoses
https://www.readbyqxmd.com/read/27423475/-antidepressant-and-tolerance-determinants-and-management-of-major-side-effects
#11
D J David, D Gourion
Antidepressant therapy aims to reach remission of depressive symptoms while reducing the complications and risks of relapse. Even though they have proven their efficacy, it takes several weeks for antidepressants to demonstrate full effectiveness, and adverse effects occur more quickly or (quicker) which can be a source of poor compliance. This latest aspect often leads to dose reduction and/or change of molecule that have the effect of delaying remission. This review attempts to present, from the pharmacological properties of the major classes of antidepressants (monoamine oxidase inhibitor [MAOI], tricyclic antidepressants [TCA], selective serotonin reuptake inhibitor [SSRI] and serotonin and noradrenaline reuptake inhibitor [SNRI]), to the pharmacological mechanisms involved in adverse effects by focusing on sexual dysfunction, nausea/vomiting, and weight changes and sleep disruption...
December 2016: L'Encéphale
https://www.readbyqxmd.com/read/27364609/development-of-cns-multi-receptor-ligands-modification-of-known-d2-pharmacophores
#12
Jagan R Etukala, Xue Y Zhu, Suresh V K Eyunni, Edem K Onyameh, Edward Ofori, Barbara A Bricker, Hye J Kang, Xi-Ping Huang, Bryan L Roth, Seth Y Ablordeppey
Several known D2 pharmacophores have been explored as templates for identifying ligands with multiple binding affinities at dopamine and serotonin receptors considered as clinically relevant receptors in the treatment of neuropsychiatric diseases. This approach has resulted in the identification of ligands that target multiple CNS receptors while avoiding others associated with deleterious effects. In particular, compounds 11, 15 and 22 may have potential for further development as antipsychotic agents as they favorably interact with the clinically relevant receptors including D2R, 5-HT1AR, and 5-HT7R...
August 15, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27317020/2-bromoterguride-a-potential-atypical-antipsychotic-drug-without-metabolic-effects-in-rats
#13
Robert T Franke, Emilia Tarland, Heidrun Fink, Heinz H Pertz, Jan Brosda
RATIONALE: Recently, we showed that 2-bromoterguride acted as a dopamine D2 receptor partial agonist, a serotonin 5-HT2A and α2C-adrenergic receptor antagonist, and exhibited antidopaminergic efficacy in amphetamine-induced locomotion (AIL) in rats without inducing catalepsy. OBJECTIVE: To extend our knowledge on the antipsychotic effects of 2-bromoterguride, we used convergent preclinical animal models and tests; i.e., conditioned avoidance response (CAR), predictive of antipsychotic-like effects; Fos protein expression, a molecular marker for (atypical) antipsychotic activity; wet dog shake behavior, a test for the in vivo effects of drugs acting on central 5-HT2A receptors; and investigated metabolic changes as a common side effect of atypical antipsychotic drugs (APDs)...
August 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27222264/current-trends-on-antipsychotics-focus-on-asenapine
#14
REVIEW
Donatella Marazziti, Armando Piccinni, Stefano Baroni, Francesco Mungai, Silvio Presta, Federico Mucci, Liliana Dell'Osso
Over the years, both first- (FGAs) and second-generation antipsychotics (SGAs), continue to gain increasing evidence of being effective in the treatment of psychotic symptoms. Currently, they represent the first-line treatment of schizophrenia and bipolar disorder, although they are widely used in psychotic depression and other clinical conditions, such as agitation and/or behavioural disturbances. Despite representing an indispensable tool for the treatment of severe psychotic disorders, they are widely known to have a number of unwanted side effects that the clinician must be aware of, and handle carefully to provide the patient the best available treatment in the short and long-term...
2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27217270/pharmacogenetic-associations-of-antipsychotic-drug-related-weight-gain-a-systematic-review-and-meta-analysis
#15
Jian-Ping Zhang, Todd Lencz, Ryan X Zhang, Masahiro Nitta, Lawrence Maayan, Majnu John, Delbert G Robinson, W Wolfgang Fleischhacker, Rene S Kahn, Roel A Ophoff, John M Kane, Anil K Malhotra, Christoph U Correll
Although weight gain is a serious but variable adverse effect of antipsychotics that has genetic underpinnings, a comprehensive meta-analysis of pharmacogenetics of antipsychotic-related weight gain is missing. In this review, random effects meta-analyses were conducted for dominant and recessive models on associations of specific single nucleotide polymorphisms (SNP) with prospectively assessed antipsychotic-related weight or body mass index (BMI) changes (primary outcome), or categorical increases in weight or BMI (≥7%; secondary outcome)...
November 2016: Schizophrenia Bulletin
https://www.readbyqxmd.com/read/27173799/synthesis-structure-activity-relationships-and-biological-evaluation-of-a-series-of-benzamides-as-potential-multireceptor-antipsychotics
#16
Feipu Yang, Xiangrui Jiang, Jianfeng Li, Yu Wang, Yongjian Liu, Minghao Bi, Chunhui Wu, Qingjie Zhao, Weiming Chen, Jingjing Yin, Jian Zhang, Yuanchao Xie, Tianwen Hu, Mingshuo Xu, Shuang Guo, Zhen Wang, Yang He, Jingshan Shen
In the present study, a series of benzamides, endowed with potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl)butoxy)-N-methylbenzamide (21) and its fluoro-substituted analogue (22) held the best pharmacological binding profiles. They not only presented potent activities for D2, 5-HT1A, and 5-HT2A receptors, but were also endowed with low activities for 5-HT2C, H1 receptors and hERG channels, suggesting a low propensity of inducing weight gain and QT prolongation...
July 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27147989/activity-of-d1-2-receptor-expressing-neurons-in-the-nucleus-accumbens-regulates-running-locomotion-and-food-intake
#17
Xianglong Zhu, David Ottenheimer, Ralph J DiLeone
While weight gain is clearly promoted by excessive energy intake and reduced expenditure, the underlying neural mechanisms of energy balance remain unclear. The nucleus accumbens (NAc) is one brain region that has received attention for its role in the regulation of energy balance; its D1 and D2 receptor containing neurons have distinct functions in regulating reward behavior and require further examination. The goal of the present study is to investigate how activation and inhibition of D1 and D2 neurons in the NAc influences behaviors related to energy intake and expenditure...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27042868/iti-007-in-the-treatment-of-schizophrenia-from-novel-pharmacology-to-clinical-outcomes
#18
Robert E Davis, Christoph U Correll
ITI-007 is an investigational drug being developed for schizophrenia and other neuropsychiatric/neurodegenerative diseases. ITI-007 has a unique pharmacological profile, combining potent 5-HT2a receptor antagonism with cell-type-specific dopamine and glutamate receptor modulation, plus serotonin reuptake inhibition. At dopamine-D2 receptors, ITI-007 acts as a post-synaptic antagonist and pre-synaptic partial agonist. Additionally, ITI-007 stimulates phosphorylation of glutamatergic NMDA-NR2B receptors, downstream of dopamine-D1 receptor intracellular signaling...
June 2016: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/27036122/lurasidone-an-antipsychotic-with-antidepressant-effects-in-bipolar-depression
#19
Nicholas A Keks, Judy Hope, David Castle
OBJECTIVE: Lurasidone is a new serotonin-dopamine antagonist atypical antipsychotic which also appears to be effective in bipolar depression. This paper will briefly review the evidence concerning lurasidone. CONCLUSIONS: Lurasidone is an antagonist at dopamine D2, serotonin 5-HT2 and 5-HT7, and partial agonist at 5HT1a receptors; it has no anticholinergic or antihistaminic activity. Rapidly absorbed, it has a half-life of 18 ± 7 hours, will reach steady state in five days and is taken at night with food (absorption is halved on an empty stomach)...
June 2016: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/26923999/-aripiprazole-gambling-disorder-and-compulsive-sexuality
#20
D Mété, C Dafreville, V Paitel, P Wind
INTRODUCTION: Aripiprazole, an atypical or second-generation antipsychotic, is usually well tolerated. It is an approved treatment for schizophrenia and mania in bipolar disorder type 1. Unlike the other antipsychotics, it has high affinity agonist properties for dopamine D2 and D3 receptors. It has also 5-HT1A partial agonist and 5-HT2A antagonist properties. Aripiprazole is a first or second line treatment frequently used because it has reduced side effects such as weight gain, sleepiness, dyslipidemia, insulin resistance, hyperprolactinemia and extrapyramidal symptoms...
June 2016: L'Encéphale
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