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https://www.readbyqxmd.com/read/29234054/antagonistic-effect-of-dopamine-structural-analogues-on-human-gaba%C3%AF-1-receptor
#1
Alfredo Alaniz-Palacios, Ataulfo Martínez-Torres
GABAergic and dopaminergic pathways are co-localized in several areas of the central nervous system and recently several reports have shown co-release of both neurotransmitters. The GABA-A receptor (β and ρ1 subunits) is modulated by dopamine (DA) and, interestingly, GABAρ1 can be modulated by several biogenic amines. Here we explored the effects of the metabolites of the dopaminergic pathway and other structural analogues of DA on GABAρ1 and the DA gated ion channel (LGC-53) from Caenorhabditis elegans expressed in Xenopus laevis oocytes...
December 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29233537/life-threatening-parkinsonism-hyperpyrexia-syndrome-following-bilateral-deep-brain-stimulation-of-the-subthalamic-nucleus
#2
Mehmet Osman Akçakaya, Nihan Hande Akçakaya, Mustafa Ömür Kasımcan, Talat Kırış
Parkinsonism-hyperpyrexia syndrome (PHS), or neuroleptic malignant syndrome (NMS), is a neurophysiologic reaction to the acute withdrawal/decrease of central dopamine levels. It is a severe complication characterized by rigidity, change in consciousness level, fever, hypertension, and autonomic instability, that can be fatal. To the best of our knowledge, PHS following deep brain stimulation (DBS) of subthalamic nucleus (STN) surgery due to anti-Parkinson drug discontinuation has been previously reported only six times...
December 6, 2017: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/29226628/modeling-of-prolactin-response-following-dopamine-d2-receptor-antagonists-in-rats-can-it-be-translated-to-clinical-dosing
#3
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride. Data on male Wistar rats receiving single or multiple doses of risperidone, paliperidone, or remoxipride was described by two semimechanistic models, the precursor pool model and the agonist-antagonist interaction model...
December 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29226617/activation-of-glucagon-like-peptide-1-receptors-in-the-nucleus-accumbens-attenuates-cocaine-seeking-in-rats
#4
Nicole S Hernandez, Bernadette O'Donovan, Pavel I Ortinski, Heath D Schmidt
Recent evidence indicates that activation of glucagon-like peptide-1 (GLP-1) receptors reduces cocaine-mediated behaviors and cocaine-evoked dopamine release in the nucleus accumbens (NAc). However, no studies have examined the role of NAc GLP-1 receptors in the reinstatement of cocaine-seeking behavior, an animal model of relapse. Here, we show that systemic infusion of a behaviorally relevant dose of the GLP-1 receptor agonist exendin-4 penetrated the brain and localized with neurons and astrocytes in the NAc...
December 11, 2017: Addiction Biology
https://www.readbyqxmd.com/read/29224383/abcb1-is-there-a-role-in-the-drug-treatment-of-parkinson-s-disease
#5
Thomas Müller
The ABCB1 (P-gp, MDR1, CD243) transporters system plays an eminent role in brain detoxification. It protects against endogenous and exogenous toxin transport into the brain parenchyma by supporting toxin efflux over the blood brain barrier. Areas covered: This editorial discusses the role and pro's and con's of ABCB1 modulation in the drug treatment of Parkinson's disease patients. Expert commentary: Experimental findings suggest that drug induced impairment of ABCB1 transporters function may improve symptomatic drug effects...
December 11, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29221778/long-term-treatment-with-dopamine-d3-receptor-agonists-induces-a-behavioral-switch-that-can-be-rescued-by-blocking-the-dopamine-d1-receptor
#6
Mai-Lynne Dinkins, Perrine Lallemand, Stefan Clemens
Restless legs syndrome (RLS) is commonly treated with the dopamine agonists pramipexole, and rotigotine, which target the inhibitory dopamine receptor subtype D3R. While initially highly effective, these compounds lose their efficacy in treating RLS over time, and long-term therapy regularly leads to a worsening of the symptoms (augmentation). This dopamine agonist-induced augmentation has become a prime concern in the treatment of RLS, and while alternate therapies are being proposed, the mechanisms leading to augmentation remain opaque...
December 2017: Sleep Medicine
https://www.readbyqxmd.com/read/29220863/a-small-dose-of-apomorphine-counteracts-the-deleterious-effects-of-middle-cerebral-artery-occlusion-in-different-models
#7
F Mastroiacovo, A Gaglione, C L Busceti, L Ryskalin, G Bozza, F Nicoletti, F Orzi, F Fornai
The present manuscript investigates in two animal species by using two different experimental models of middle cerebral artery occlusion (permanent and transient), the neuroprotective effects of the dopamine receptor agonist apomorphine. These effects were evaluated by measuring the infarct volume and by counting muscle strength at different time points following the ischemic insult. Apomorphine at the dose of 3 mg/Kg when adminsitered at two hours following the occlusion of the middle cerebral artery was able to reduce significantly the infarct volume in the cortex of mice and the ischemic volume of the basal ganglia perfused by the perforant branches of the middle cerebral artery in the rat...
September 1, 2017: Archives Italiennes de Biologie
https://www.readbyqxmd.com/read/29216450/endocannabinoid-actions-on-cortical-terminals-orchestrate-local-modulation-of-dopamine-release-in-the-nucleus-accumbens
#8
Yolanda Mateo, Kari A Johnson, Dan P Covey, Brady K Atwood, Hui-Ling Wang, Shiliang Zhang, Iness Gildish, Roger Cachope, Luigi Bellocchio, Manuel Guzmán, Marisela Morales, Joseph F Cheer, David M Lovinger
Dopamine (DA) transmission mediates numerous aspects of behavior. Although DA release is strongly linked to firing of DA neurons, recent developments indicate the importance of presynaptic modulation at striatal dopaminergic terminals. The endocannabinoid (eCB) system regulates DA release and is a canonical gatekeeper of goal-directed behavior. Here we report that extracellular DA increases induced by selective optogenetic activation of cholinergic neurons in the nucleus accumbens (NAc) are inhibited by CB1 agonists and eCBs...
December 6, 2017: Neuron
https://www.readbyqxmd.com/read/29209406/serum-prolactin-levels-and-sexual-dysfunction-in-patients-with-schizophrenia-treated-with-antipsychotics-comparison-between-aripiprazole-and-other-atypical-antipsychotics
#9
Eiji Kirino
Objectives: Antipsychotics, even atypical ones, can induce hyperprolactinemia. Aripiprazole (APZ), a dopamine D2 partial agonist, has a unique pharmacological profile and few side effects. We investigated the incidence of hyperprolactinemia in patients with schizophrenia treated with APZ and other antipsychotics. Methods: Serum prolactin levels were measured by ELISA (enzyme-linked immunosorbent assay). A questionnaire survey was used to evaluate subjective sexual dysfunction...
2017: Annals of General Psychiatry
https://www.readbyqxmd.com/read/29208364/dopamine-promotes-cellular-iron-accumulation-and-oxidative-stress-responses-in-macrophages
#10
Stefanie Dichtl, David Haschka, Manfred Nairz, Markus Seifert, Chiara Volani, Oliver Lutz, Günter Weiss
Iron is essential for many biological functions including neurotransmitter synthesis, where the metal is a co-factor of tyrosine hydroxylase, which converts tyrosine to dopamine and further to norepinephrine. As the shared chemical structure, called catechol, may potentially bind iron we questioned whether tyrosine derived hormones would impact on cellular iron homeostasis in macrophages, which are central for the maintenance of body iron homeostasis. Using murine bone marrow-derived macrophages (BMDMs), we investigated the effect of catecholamines and found that only dopamine but neither tyrosine, nor norepinephrine, affected cellular iron homeostasis...
December 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29206881/deletion-of-lynx1-reduces-the-function-of-%C3%AE-6-nicotinic-receptors
#11
Rell L Parker, Heidi C O'Neill, Beverley M Henley, Charles R Wageman, Ryan M Drenan, Michael J Marks, Julie M Miwa, Sharon R Grady, Henry A Lester
The α6 nicotinic acetylcholine receptor (nAChR) subunit is an attractive drug target for treating nicotine addiction because it is present at limited sites in the brain including the reward pathway. Lynx1 modulates several nAChR subtypes; lynx1-nAChR interaction sites could possibly provide drug targets. We found that dopaminergic cells from the substantia nigra pars compacta (SNc) express lynx1 mRNA transcripts and, as assessed by co-immunoprecipitation, α6 receptors form stable complexes with lynx1 protein, although co-transfection with lynx1 did not affect nicotine-induced currents from cell lines transfected with α6 and β2...
2017: PloS One
https://www.readbyqxmd.com/read/29204312/insights-into-pathophysiology-from-medication-induced-tremor
#12
REVIEW
John C Morgan, Julie A Kurek, Jennie L Davis, Kapil D Sethi
Background: Medication-induced tremor (MIT) is common in clinical practice and there are many medications/drugs that can cause or exacerbate tremors. MIT typically occurs by enhancement of physiological tremor (EPT), but not all drugs cause tremor in this way. In this manuscript, we review how some common examples of MIT have informed us about the pathophysiology of tremor. Methods: We performed a PubMed literature search for published articles dealing with MIT and attempted to identify articles that especially dealt with the medication's mechanism of inducing tremor...
2017: Tremor and Other Hyperkinetic Movements
https://www.readbyqxmd.com/read/29204126/pharmacokinetic-ambulatory-and-hyperthermic-effects-of-3-4-methylenedioxy-n-methylcathinone-methylone-in-rats
#13
Kristýna Štefková, Monika Židková, Rachel R Horsley, Nikola Pinterová, Klára Šíchová, Libor Uttl, Marie Balíková, Hynek Danda, Martin Kuchař, Tomáš Páleníček
Methylone (3,4-methylenedioxy-N-methylcathinone) is a synthetic cathinone analog of the recreational drug ecstasy. Although it is marketed to recreational users as relatively safe, fatalities due to hyperthermia, serotonin syndrome, and multi-organ system failure have been reported. Since psychopharmacological data remain scarce, we have focused our research on pharmacokinetics, and on a detailed evaluation of temporal effects of methylone and its metabolite nor-methylone on behavior and body temperature in rats...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29201667/the-effects-of-adjuvant-therapies-on-embryo-transfer-success
#14
Rachael Shirlow, Martin Healey, Michelle Volovsky, Vivien MacLachlan, Beverley Vollenhoven
Background: Many adjuvant therapies are employed during IVF treatment in an attempt to improve outcomes. The objective of our study was to evaluate the impact of thirteen adjuvants (Intralipid, steroids, melatonin, coenzyme Q10, Filgrastim, testosterone, DHEA, growth hormone, antibiotics, hCG infusion, aspirin, enoxaparin/heparin and dopamine agonists) on the success of embryo transfers. Methods: This is a retrospective cohort study of all embryo transfers between January 2010 and April 2015 from a multi-site IVF clinic...
October 2017: Journal of Reproduction & Infertility
https://www.readbyqxmd.com/read/29198512/understanding-the-role-of-serotonin-in-female-hypoactive-sexual-desire-disorder-and-treatment-options
#15
REVIEW
Harry A Croft
BACKGROUND: The neurobiology of sexual response is driven in part by dopamine and serotonin-the former modulating excitatory pathways and the latter regulating inhibitory pathways. Neurobiological underpinnings of hypoactive sexual desire disorder (HSDD) are seemingly related to overactive serotonin activity that results in underactive dopamine activity. As such, pharmacologic agents that decrease serotonin, increase dopamine, or some combination thereof, have therapeutic potential for HSDD...
December 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29194070/changes-in-gut-microbiota-during-development-of-compulsive-checking-and-locomotor-sensitization-induced-by-chronic-treatment-with-the-dopamine-agonist-quinpirole
#16
Tony D Jung, Paul S Jung, Lucshman Raveendran, Yasamin Farbod, Anna Dvorkin-Gheva, Boris Sakic, Michael G Surette, Henry Szechtman
Long-term treatment of rats with the D2/D3 dopamine agonist quinpirole induces compulsive checking (proposed as animal model of obsessive-compulsive disorder) and locomotor sensitization. The mechanisms by which long-term use of quinpirole produces those behavioral transformations are not known. Here we examined whether changes in gut microbiota play a role in these behavioral phenomena ηP, by monitoring the development of compulsive checking and locomotor sensitization at the same time as measuring the response of gut microbiota to chronic quinpirole injections...
November 29, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29191406/enantioselective-separation-of-racemates-using-chiralpak-ig-amylose-based-chiral-stationary-phase-under-normal-standard-non-standard-and-reversed-phase-high-performance-liquid-chromatography
#17
Ashraf Ghanem, Chexu Wang
We have previously reported on the solvent versatility of immobilized amylose and cellulose-based chiral stationary phases in enantioselective liquid chromatographic separation of racemates. The studies were mainly focusing on the tris substituted 3,5-dimethylphenylcarbamate polysaccharide-based chiral stationary phases namely CHIRALPAK IA® [Amylose tris (3,5-dimethylphenylcarbamate)] or ADMPC and CHIRALPAK IB® [Cellulose tris (3,5-dimethylphenylcarbamate)] or CDMPC. Here we focus on the application of the recently introduced amylose tris (3-chloro-5-methylphenylcarbamate) or ACMPC and brand name CHIRALPAK IG® with a chlorine substituent replacing the methyl group in CHIRALPAK IA®...
November 24, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29189169/computer-aided-drug-design-applied-to-parkinson-targets
#18
Hamilton M Ishiki, Jose Maria Barbosa Filho, Marcelo S da Silva, Marcus T Scotti, Luciana Scotti
Parkinson's disease (PD) is a progressive neurodegenerative disorder characterized by debilitating motor deficits, as well as autonomic problems, cognitive declines, changes in affect and sleep disturbances. Although the scientific community has performed great efforts in the study of PD, and from the most diverse points of view, the disease remains incurable. The exact mechanism underlying its progression is unclear, but oxidative stress, mitochondrial dysfunction and inflammation are thought to play major roles in the etiology...
November 28, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/29187755/a-mouse-model-of-the-schizophrenia-associated-1q21-1-microdeletion-syndrome-exhibits-altered-mesolimbic-dopamine-transmission
#19
Jacob Nielsen, Kim Fejgin, Florence Sotty, Vibeke Nielsen, Arne Mørk, Claus T Christoffersen, Leonid Yavich, Jes B Lauridsen, Dorte Clausen, Peter H Larsen, Jan Egebjerg, Thomas M Werge, Pekka Kallunki, Kenneth V Christensen, Michael Didriksen
1q21.1 hemizygous microdeletion is a copy number variant leading to eightfold increased risk of schizophrenia. In order to investigate biological alterations induced by this microdeletion, we generated a novel mouse model (Df(h1q21)/+) and characterized it in a broad test battery focusing on schizophrenia-related assays. Df(h1q21)/+ mice displayed increased hyperactivity in response to amphetamine challenge and increased sensitivity to the disruptive effects of amphetamine and phencyclidine hydrochloride (PCP) on prepulse inhibition...
November 30, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/29180135/alpha-synuclein-transgenic-mice-h-%C3%AE-synl62-display-%C3%AE-syn-aggregation-and-a-dopaminergic-phenotype-reminiscent-of-parkinson-s-disease
#20
Silke Frahm, Valeria Melis, David Horsley, Janet E Rickard, Gernot Riedel, Paula Fadda, Maria Scherma, Charles R Harrington, Claude M Wischik, Franz Theuring, Karima Schwab
Alpha-Synuclein (α-Syn) accumulation is considered a major risk factor for the development of synucleinopathies such as Parkinson's disease (PD) and dementia with Lewy bodies. We have generated mice overexpressing full-length human α-Syn fused to a membrane-targeting signal sequence under the control of the mouse Thy1-promotor. Three separate lines (L56, L58 and L62) with similar gene expression levels, but considerably heightened protein accumulation in L58 and L62, were established. In L62, there was widespread labelling of α-Syn immunoreactivity in brain including spinal cord, basal forebrain, cortex and striatum...
November 24, 2017: Behavioural Brain Research
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