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Dopamine antagonists

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https://www.readbyqxmd.com/read/29154107/aripiprazole-in-treatment-of-gilles-de-la-tourette-syndrome-new-therapeutic-option
#1
REVIEW
Piotr Janik, Natalia Szejko
Aripiprazole is a dopamine D2- and serotonin 5-hydroxytryptamine (5-HT)1A receptor partial agonist and 5-HT2A receptor antagonist primarily used for the treatment of schizophrenia, bipolar disorder or depression with psychotic ideation. However, recently a number of new possible indications have been suggested, among them Gilles de la Tourette syndrome (GTS). In two randomized, double-blind, placebo-controlled studies in children and adolescents with GTS has been confirmed the efficacy of aripiprazole in tic reduction...
November 9, 2017: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/29146502/protracted-motivational-dopamine-related-deficits-following-adolescence-sugar-overconsumption
#2
Fabien Naneix, Florence Darlot, Véronique De Smedt-Peyrusse, Jean-Rémi Pape, Etienne Coutureau, Martine Cador
Adolescence represents a critical period characterized by major neurobiological changes. Chronic stimulation of the reward system during adolescence might constitute an important factor of vulnerability to pathological development. Increasing evidences suggest that adolescent overconsumption of sweet palatable foods impact reward-based processes. However, the neurobiological bases of these deficits remain poorly understood. Previous studies have demonstrated motivational deficits for palatable foods after sweet diet exposure during adolescence that might involve the dopamine (DA) system, a central actor in incentive processes...
November 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29139159/syntaxin1b-contributes-to-regulation-of-the-dopaminergic-system-through-gaba-transmission-in-the-cns
#3
Tomonori Fujiwara, Takefumi Kofuji, Tatsuya Mishima, Kimio Akagawa
In neuronal plasma membrane, two syntaxin isoforms, HPC-1/syntaxin1A (STX1A) and syntaxin1B (STX1B), are predominantly expressed as soluble N-ethylmaleimide-sensitive fusion attachment protein receptors, also known as t-SNAREs. We previously reported that glutamatergic and GABAergic synaptic transmission is impaired in Stx1b null mutant (Stx1b(-/-) ) mice, but is almost normal in Stx1a null mutant (Stx1a(-/-) ) mice. These observations suggested that STX1A and STX1B have distinct functions in fast synaptic transmission in the central nervous system (CNS)...
November 15, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29139105/preoperative-medical-therapy-before-surgery-for-uterine-fibroids
#4
REVIEW
Anne Lethaby, Lucian Puscasiu, Beverley Vollenhoven
BACKGROUND: Uterine fibroids occur in up to 40% of women aged over 35 years. Some are asymptomatic, but up to 50% cause symptoms that warrant therapy. Symptoms include anaemia caused by heavy menstrual bleeding, pelvic pain, dysmenorrhoea, infertility and low quality of life. Surgery is the first choice of treatment. In recent years, medical therapies have been used before surgery to improve intraoperative and postoperative outcomes. However, such therapies tend to be expensive.Fibroid growth is stimulated by oestrogen...
November 15, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29137945/the-effects-of-local-microinjection-of-selective-dopamine-d1-and-d2-receptor-agonists-and-antagonists-into-the-dorsal-raphe-nucleus-on-sleep-and-wakefulness-in-the-rat
#5
Jaime M Monti, Héctor Jantos
The effects of the dopamine (DA) D1 and D2 receptor agonists SKF38393, bromocriptine and quinpirole, respectively, on spontaneous sleep were analyzed in adult rats prepared for chronic sleep recordings. Local administration of the DAergic agonists into the dorsal raphe nucleus (DRN) during the light phase of the light-dark cycle induced a significant reduction of rapid-eye movement sleep (REMS) and the number of REM periods. Additionally, bromocriptine and quinpirole significantly increased wakefulness (W)...
November 11, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29135937/relax-cool-down-and-scaffold-how-to-restore-surface-expression-of-folding-deficient-mutant-gpcrs-and-slc6-transporters
#6
REVIEW
H M Mazhar Asjad, Shahrooz Nasrollahi-Shirazi, Sonja Sucic, Michael Freissmuth, Christian Nanoff
Many diseases arise from mutations, which impair protein folding. The study of folding-deficient variants of G protein-coupled receptors and solute carrier 6 (SLC6) transporters has shed light on the folding trajectory, how it is monitored and how misfolding can be remedied. Reducing the temperature lowers the energy barrier between folding intermediates and thereby eliminates stalling along the folding trajectory. For obvious reasons, cooling down is not a therapeutic option. One approach to rescue misfolded variants is to use membrane-permeable orthosteric ligands...
November 14, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29134560/neurochemical-and-neurotoxic-effects-of-mdma-ecstasy-and-caffeine-after-chronic-combined-administration-in-mice
#7
Anna Maria Górska, Katarzyna Kamińska, Agnieszka Wawrzczak-Bargieła, Giulia Costa, Micaela Morelli, Ryszard Przewłocki, Grzegorz Kreiner, Krystyna Gołembiowska
MDMA (3,4-methylenedioxymethamphetamine) is a psychostimulant popular as a recreational drug because of its effect on mood and social interactions. MDMA acts at dopamine (DA) transporter (DAT) and serotonin (5-HT) transporter (SERT) and is known to induce damage of dopamine and serotonin neurons. MDMA is often ingested with caffeine. Caffeine as a non-selective adenosine A1/A2A receptor antagonist affects dopaminergic and serotonergic transmissions. The aim of the present study was to determine the changes in DA and 5-HT release in the mouse striatum induced by MDMA and caffeine after their chronic administration...
November 13, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29132050/cannabinoid-hyperemesis-syndrome-review-of-the-literature-and-of-cases-reported-to-the-french-addictovigilance-network
#8
REVIEW
Benoît Schreck, Nicolas Wagneur, Pascal Caillet, Marie Gérardin, Jennyfer Cholet, Michel Spadari, Nicolas Authier, Juliana Tournebize, Marion Gaillard, Anais Serre, Louise Carton, Stéphanie Pain, Pascale Jolliet, Caroline Victorri-Vigneau
BACKGROUND: Cannabinoid hyperemesis syndrome is a variant of cyclical vomiting syndrome in a context of chronic cannabis usage. Our aim was to compare French cases to those identified in the international literature in order to further our knowledge of the clinical criteria, pathophysiology and treatments for cannabinoid hyperemesis syndrome. METHODS: We analysed cases reported in the international literature up to 30 June 2017, obtained from the MEDLINE, PsycINFO and The Cochrane Library databases; we selected relevant articles based on title and abstract...
November 7, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#9
Theresa Mallick-Searle, Mechele Fillman
PURPOSE: Opioid medications are integral in managing acute moderate-to-severe pain. Opioid analgesics bind to μ (mu), κ (kappa), or δ (delta) opioid receptors in the brain, spinal cord, and digestive tract. However, opioids cause adverse effects that may interfere with their therapeutic use. Some adverse effects wane over time, but patients using opioids for acute pain struggle with opioid-induced nausea and vomiting (OINV) the entire time they take the opioid. This article discusses the underlying mechanisms, clinical implications, and treatment strategies of OINV...
November 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/29128806/emotional-disorders-induced-by-hemopressin-and-rvd-hemopressin-%C3%AE-administration-in-rats
#10
Sheila Leone, Lucia Recinella, Annalisa Chiavaroli, Sara Martinotti, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Szabolcs Dvorácskó, Csaba Tömböly, Luciano De Petrocellis, Michele Vacca, Luigi Brunetti, Giustino Orlando
BACKGROUND: The endocannabinoid (eCB) system plays an important role in regulating emotional disorders, and is involved, directly or indirectly, in psychiatric diseases, such as anxiety and depression. Hemopressin, a hemoglobin α chain-derived peptide, and RVD-hemopressin(α), a N-terminally extended form of hemopressin, act as antagonist/inverse agonist and negative allosteric modulator of the cannabinoid 1 (CB1) receptor, respectively. METHODS: Considering the possible involvement of these peptides on emotional behaviour, the aim of our study was to investigate the behavioural effects of a single intraperitoneal (ip) injection of hemopressin (0...
June 23, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128790/the-antipsychotic-like-effects-in-rodents-of-yqa31-involve-dopamine-d3-and-5-ht1a-receptor
#11
Hong-Yan Gou, Xue Sun, Fei Li, Zhi-Yuan Wang, Ning Wu, Rui-Bin Su, Bin Cong, Jin Li
BACKGROUND: We previously reported that YQA31 is a dopamine D3 receptor antagonist with modest 5-HT1A receptor affinity and that it exhibits antipsychotic properties in animal models of schizophrenia. However, the contributions of D3 and 5-HT1A receptors in the anti-psychotic effects of YQA31 are not clear. The current study evaluated the role of these two receptors in the effect of YQA31 on the hyperactivity and novel object recognition deficit in mice. METHODS: We used dopamine D3 receptor knockout mice and 5-HT1A receptor antagonist WAY100635 pretreatment, respectively, to investigate the involvement of these receptors in the effects of YQA31...
May 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128392/adrenergic-manipulation-inhibits-pavlovian-conditioned-approach-behaviors
#12
Kyle Z Pasquariello, Marina Han, Cagla Unal, Paul J Meyer
Environmental rewards and Pavlovian reward cues can acquire incentive salience, thereby eliciting incentive motivational states and instigate reward-seeking. In rats, the incentive salience of food cues can be measured during a Pavlovian conditioned approach paradigm, in which rats engage in cue-directed approach ("sign-tracking") or approach the food delivery location ("goal-tracking"). While it has been shown that dopamine signaling is necessary for sign-tracking, some studies have suggested that norepinephrine is involved in learning to sign-track as well...
November 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29125762/highly-selective-dopamine-d3-receptor-antagonists-with-arylated-diazaspiro-alkane-cores
#13
Sean W Reilly, Suzy Griffin, Michelle Taylor, Kristoffer Sahlholm, Chi-Chang Weng, Kuiying Xu, Daniel A Jacome, Robert R Luedtke, Robert H Mach
A series of potent and selective D3 receptor (D3R) analogues with diazaspiro alkane cores were synthesized. Radioligand binding of compounds 11, 14, 15a, and 15c revealed favorable D3R affinity (Ki = 12-25.6 nM) and were highly selective for D3R vs D3R (ranging from 264-905-fold). Variation of these novel ligand architectures can be achieved using our previously reported 10-20 minute benchtop C-N cross-coupling methodology, affording a broad range of arylated diazaspiro pre-cursors.
November 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29120551/current-medical-strategies-in-the-prevention-of-ovarian-hyperstimulation-syndrome
#14
Miro Kasum, Slavko Orešković, Daniela Franulić, Ermin Čehić, Albert Lila, Goran Vujić, Franjo Grgić
The purpose of this review is to analyze current medical strategies in the prevention of ovarian hyperstimulation syndrome (OHSS) during ovarian stimulation for in vitro fertilization. Owing to contemporary preventive measures of OHSS, the incidence of moderate and severe forms of the syndrome varies between 0.18% and 1.40%. Although none of medical strategies is completely effective, there is high-quality evidence that replacing human chorionic gonadotropin (hCG) by gonadotropin-releasing hormone (GnRH) agonists after GnRH antagonists and moderate- quality evidence that GnRH antagonist protocols, dopamine agonists and mild protocols reduce the occurrence of OHSS...
March 2017: Acta Clinica Croatica
https://www.readbyqxmd.com/read/29119585/effects-of-dopamine-receptor-antagonist-antipsychotic-therapy-on-blood-pressure
#15
REVIEW
N H Gonsai, V H Amin, C G Mendpara, R Speth, G M Hale
WHAT IS KNOWN AND OBJECTIVE: Hypertension, a major risk factor for adverse cardiovascular events, such as stroke and myocardial infarction, affects 80 million American adults. The aetiology of hypertension is multifaceted and difficult to identify. Dopamine receptors, especially those in the kidneys, play a role in blood pressure regulation, and alterations in their function can cause hypertension. The objective of this review was to investigate the association between the use of dopamine antagonists with hypertension focusing especially on second-generation antipsychotics, like clozapine that is D4 receptor antagonist...
November 8, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/29109060/cannabinoid-1-receptor-neutral-antagonist-reduces-binge-like-alcohol-consumption-and-alcohol-induced-accumbal-dopaminergic-signaling
#16
Andrea Balla, Bin Dong, Borehalli M Shilpa, Kiran Vemuri, Alexandros Makriyannis, Subhash C Pandey, Henry Sershen, Raymond F Suckow, K Yaragudri Vinod
Binge alcohol (ethanol) drinking is associated with profound adverse effects on our health and society. Rimonabant (SR141716A), a CB1 receptor inverse agonist, was previously shown to be effective for nicotine cessation and obesity. However, studies using rimonabant were discontinued as it was associated with an increased risk of depression and anxiety. In the present study, we examined the pharmacokinetics and effects of AM4113, a novel CB1 receptor neutral antagonist on binge-like ethanol drinking in C57BL/6J mice using a two-bottle choice drinking-in-dark (DID) paradigm...
November 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29107956/estradiol-increases-the-sensitivity-of-ventral-tegmental-area-dopamine-neurons-to-dopamine-and-ethanol
#17
Bertha J Vandegrift, Chang You, Rosalba Satta, Mark S Brodie, Amy W Lasek
Gender differences in psychiatric disorders such as addiction may be modulated by the steroid hormone estrogen. For instance, 17β-estradiol (E2), the predominant form of circulating estrogen in pre-menopausal females, increases ethanol consumption, suggesting that E2 may affect the rewarding properties of ethanol and thus the development of alcohol use disorder in females. The ventral tegmental area (VTA) is critically involved in the rewarding and reinforcing effects of ethanol. In order to determine the role of E2 in VTA physiology, gonadally intact female mice were sacrificed during diestrus II (high E2) or estrus (low E2) for electrophysiology recordings...
2017: PloS One
https://www.readbyqxmd.com/read/29107444/dopamine-d2l-receptor-interacting-proteins-regulate-dopaminergic-signaling
#18
REVIEW
Norifumi Shioda
Dopamine receptor family proteins include seven transmembrane and trimeric GTP-binding protein-coupled receptors (GPCRs). Among them, the dopamine D2 receptor (D2R) is most extensively studied. All clinically used antipsychotic drugs serve as D2R antagonists in the mesolimbic dopamine system, and their ability to block D2R signaling is positively correlated with antipsychotic efficiency. Human genetic studies also show a significant association of DRD2 polymorphisms with disorders including schizophrenia and Parkinson's disease...
October 14, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29106979/development-of-a-population-pharmacokinetic-model-to-predict-brain-distribution-and-dopamine-d2-receptor-occupancy-of-raclopride-in-non-anesthetized-rat
#19
Yin Cheong Wong, Trayana Ilkova, Rob C van Wijk, Robin Hartman, Elizabeth C M de Lange
BACKGROUND: Raclopride is a selective antagonist of the dopamine D2 receptor. It is one of the most frequently used in vivo D2 tracers (at low doses) for assessing drug-induced receptor occupancy (RO) in animals and humans. It is also commonly used as a pharmacological blocker (at high doses) to occupy the available D2 receptors and antagonize the action of dopamine or drugs on D2 in preclinical studies. The aims of this study were to comprehensively evaluate its pharmacokinetic (PK) profiles in different brain compartments and to establish a PK-RO model that could predict the brain distribution and RO of raclopride in the freely moving rat using a LC-MS based approach...
November 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29097596/ck2-oppositely-modulates-l-dopa-induced-dyskinesia-via-striatal-projection-neurons-expressing-d1-or-d2-receptors
#20
Marisol Cortés, Lauren Malave, Julia Castello, Marc Flajolet, M Angela Cenci, Eitan Friedman, Heike Rebholz
We have previously shown that casein kinase 2 (CK2) negatively regulates dopamine D1- and adenosine A2a receptor signaling in the striatum. Ablation of CK2 in D1-receptor-positive striatal neurons caused enhanced locomotion and exploration at baseline, whereas CK2 ablation in D2 receptor-positive neurons caused increased locomotion after treatment with A2a antagonist, caffeine. Since both, D1 and A2a receptors, play major roles in the cellular responses to L-DOPA in the striatum, these findings prompted us to examine the impact of CK2 ablation on the effects of L-DOPA treatment in the unilateral 6-OHDA lesioned mouse model of Parkinson's disease...
November 2, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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