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Dopamine antagonists

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https://www.readbyqxmd.com/read/27902847/food-deprivation-facilitates-reinstatement-of-morphine-induced-conditioned-place-preference-role-of-intra-accumbal-dopamine-d2-like-receptors-in-associating-reinstatement-of-morphine-cpp-with-stress
#1
Fatemeh Sadeghzadeh, Vahab Babapour, Abbas Haghparast
The high rate of relapse to drug use is one of the main problems in the treatment of addiction. Stress plays the essential role in drug abuse and relapse; nevertheless, little is known about the mechanisms underlying stress and relapse. Accordingly, the effects of intra-accumbal administration of Sulpiride, as a dopamine D2-like receptor antagonist, on an ineffective morphine dose+food deprivation(FD)- and morphine priming-induced reinstatement of conditioned place preference (CPP). 104 adult male albino Wistar rats weighing 200-280g were bilaterally implanted by cannula into the nucleus accumbens (NAc)...
November 30, 2016: Synapse
https://www.readbyqxmd.com/read/27902493/intravenous-amisulpride-for-the-prevention-of-postoperative-nausea-and-vomiting-two-concurrent-randomized-double-blind-placebo-controlled-trials
#2
Tong J Gan, Peter Kranke, Harold S Minkowitz, Sergio D Bergese, Johann Motsch, Leopold Eberhart, David G Leiman, Timothy I Melson, Dominique Chassard, Anthony L Kovac, Keith A Candiotti, Gabriel Fox, Pierre Diemunsch
BACKGROUND: Two essentially identical, randomized, double-blind, placebo-controlled, parallel-group phase III studies evaluated the efficacy of intravenous amisulpride, a dopamine D2/D3 antagonist, in the prevention of postoperative nausea and vomiting in adult surgical patients. METHODS: Adult inpatients undergoing elective surgery during general anesthesia and having at least two of the four Apfel risk factors for postoperative nausea and vomiting were enrolled at 9 U...
November 30, 2016: Anesthesiology
https://www.readbyqxmd.com/read/27894877/relief-learning-requires-a-coincident-activation-of-dopamine-d1-and-nmda-receptors-within-the-nucleus-accumbens
#3
Jorge R Bergado Acosta, Evelyn Kahl, Georgios Kogias, Taygun C Uzuneser, Markus Fendt
Relief learning is the association of a stimulus with the offset of an aversive event. Later, the now conditioned relief stimulus induces appetitive-like behavioral changes. We previously demonstrated that the NMDA receptors within the nucleus accumbens (NAC) are involved in relief learning. The NAC is also important for reward learning and it has been shown that reward learning is mediated by an interaction of accumbal dopamine and NMDA glutamate receptors. Since conditioned relief has reward-like properties, we hypothesized that (a) acquisition of relief learning requires the activation of dopamine D1 receptors in the NAC, and (b) if D1 receptors are involved in this process as expected, a concurrent dopamine D1 and NMDA receptor activation may mediate this learning...
November 25, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27885812/a-whole-animal-chemical-screen-approach-to-identify-modifiers-of-intestinal-neutrophilic-inflammation
#4
Stefan H Oehlers, Maria Vega Flores, Christopher J Hall, Liuyang Wang, Dennis C Ko, Kathryn E Crosier, Philip S Crosier
By performing two high-content small molecule screens on DSS- and TNBS-induced zebrafish enterocolitis models of inflammatory bowel disease, we have identified novel anti-inflammatory drugs from the John Hopkins Clinical Compound Library that suppress neutrophilic inflammation. Live imaging of neutrophil distribution was used to assess the level of acute inflammation and concurrently screen for off-target drug effects. Supporting the validity of our screening strategy, most of the anti-inflammatory drug hits were known antibiotics or anti-inflammatory agents...
November 25, 2016: FEBS Journal
https://www.readbyqxmd.com/read/27872762/understanding-the-functional-plasticity-in-neural-networks-of-the-basal-ganglia-in-cocaine-use-disorder-a-role-for-allosteric-receptor-receptor-interactions-in-a2a-d2-heteroreceptor-complexes
#5
REVIEW
Dasiel O Borroto-Escuela, Karolina Wydra, Julia Pintsuk, Manuel Narvaez, Fidel Corrales, Magdalena Zaniewska, Luigi F Agnati, Rafael Franco, Sergio Tanganelli, Luca Ferraro, Malgorzata Filip, Kjell Fuxe
Our hypothesis is that allosteric receptor-receptor interactions in homo- and heteroreceptor complexes may form the molecular basis of learning and memory. This principle is illustrated by showing how cocaine abuse can alter the adenosine A2AR-dopamine D2R heterocomplexes and their receptor-receptor interactions and hereby induce neural plasticity in the basal ganglia. Studies with A2AR ligands using cocaine self-administration procedures indicate that antagonistic allosteric A2AR-D2R heterocomplexes of the ventral striatopallidal GABA antireward pathway play a significant role in reducing cocaine induced reward, motivation, and cocaine seeking...
2016: Neural Plasticity
https://www.readbyqxmd.com/read/27872695/reduction-of-the-morphine-maintenance-by-blockade-of-the-nmda-receptors-during-extinction-period-in-conditioned-place-preference-paradigm-of-rats
#6
Ali Siahposht-Khachaki, Zahra Fatahi, Abbas Haghparast
INTRODUCTION: Activation of N-methyl-d-aspartate (NMDA) glutamate receptors in the nucleus accumbens is a component of drug-induced reward mechanism. In addition, NMDA receptors play a major role in brain reward system and activation of these receptors can change firing pattern of dopamine neurons. Blockade of glutamatergic neurotransmission reduces the expression of conditioned place preference (CPP) induced by morphine. Therefore, in this study, by using an NMDA receptor antagonist, DL-2-Amino-5-phosphonopentanoic acid sodium salt (AP5), the role of NMDA receptors on the maintenance and reinstatement of morphine-CPP was investigated...
October 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27870780/the-activation-of-metabotropic-glutamate-5-receptors-in-the-rat-ventral-tegmental-area-increases-dopamine-extracellular-levels
#7
Carla Ferrada, Ramón Sotomayor-Zárate, Jorge Abarca, Katia Gysling
The mesocorticolimbic circuit projects to the prefrontal cortex, hippocampus, amygdala, and nucleus accumbens, among others, and it originates in the dopaminergic neurons of the ventral tegmental area (VTA). The VTA receives glutamatergic inputs from the prefrontal cortex and several subcortical regions. The glutamate released activates dopaminergic neurons and its action depends on the activation of ionotropic and metabotropic glutamate receptors. VTA dopaminergic neurons release dopamine (DA) from axon terminals in the innervated regions and somatodendritically in the VTA itself...
January 1, 2017: Neuroreport
https://www.readbyqxmd.com/read/27865867/d1-like-dopamine-receptor-dysfunction-in-the-lateral-habenula-nucleus-increased-anxiety-like-behavior-in-rat
#8
Jiangping Chan, Yiling Ni, Pengyue Zhang, Yanmei Chen, Jichuan Zhang
Lateral habenula (LHb) is important for emotional processing. It is a link node between forebrain and midbrain. LHb is reciprocally connected with ventral tegmental area, acting as a regulatory center for the dopaminergic system. However, the role of dopamine receptors in the LHb in emotional processing is less clear. In the present study, the expression of dopamine D1 and D2 receptors in LHb was testified by western blot. In addition, D1- or D2-like receptor agonist or antagonist was bilaterally administered into the LHb, anxiety-like and depressive-like behaviors were tested 15min later in rats...
November 16, 2016: Neuroscience
https://www.readbyqxmd.com/read/27862283/footshock-induced-plasticity-of-gabab-signalling-in-the-lateral-habenula-requires-dopamine-and-glucocorticoid-receptors
#9
Salvatore Lecca, Massimo Trusel, Manuel Mameli
The activity of lateral habenula (LHb) represents a substrate for the encoding of negative-valenced events. The exposure to aversive stimuli in naïve mice is sufficient to trigger a reduction in GABAB -mediated signaling in the LHb. This is ultimately instrumental for the hyperactivity of LHb neurons and for the establishment of depressive-like phenotypes. However, the mechanisms responsible for the induction of this aversion-driven plasticity are missing. Using ex-vivo patch-clamp recordings in slices, here we show that exposing mice to a series of inescapable footshocks (FsE) rapidly reduces baclofen-mediated GABAB currents in the LHb...
November 10, 2016: Synapse
https://www.readbyqxmd.com/read/27853928/d1-and-d2-specific-dopamine-antagonist-modulate-the-caudate-nucleus-neuronal-responses-to-chronic-methylphenidate-exposure
#10
Sidish Venkataraman, Catherine Claussen, Nachum Dafny
The psychostimulant, methylphenidate (MPD), is the first line treatment as a pharmacotherapy to treat behavioral disorders such as attention deficit hyperactivity disorder (ADHD). MPD is commonly misused in non-ADHD (normal) youth and young adults both as a recreational drug and for cognitive enhancing effects to improve their grades. MPD is known to act on the reward circuit; including the caudate nucleus (CN). The CN is comprised of medium spiny neurons containing largely dopamine (DA) D1 and D2 receptors...
November 16, 2016: Journal of Neural Transmission
https://www.readbyqxmd.com/read/27851908/n-phenylpropyl-n-substituted-piperazines-occupy-sigma-receptors-and-alter-methamphetamine-induced-hyperactivity-in-mice
#11
Dennis K Miller, Eric S Park, Susan Z Lever, John R Lever
This study examined the effect of the N-phenylpropyl-N'-substituted piperazine ligands SA4503 (3.4-dimethoxyphenethyl), YZ-067 (4-methoxyphenethyl), YZ-185 (3-methoxyphenethyl) and Nahas-3h (4-methoxybenzyl) on methamphetamine-induced hyperactivity in mice. In a previous study in rats, SA4503 increased methamphetamine-induced hyperactivity at a lower ligand dose and enhanced it at a higher dose. The other ligands have not been investigated in this assay. Presently, mice were administered sigma ligands, and specific [(125)I]E-IA-DM-PE-PIPZE and [(125)I]RTI-121 binding was measured to determine σ1 sigma receptor and dopamine transporter occupancy, respectively...
November 13, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27845229/chronic-restraint-stress-causes-a-delayed-increase-in-responding-for-palatable-food-cues-during-forced-abstinence-via-a-dopamine-d1-like-receptor-mediated-mechanism
#12
Kevin T Ball, Olivia Best, Jonathan Luo, Leah R Miller
Relapse to unhealthy eating habits in dieters is often triggered by stress. Animal models, moreover, have confirmed a causal role for acute stress in relapse. The role of chronic stress in relapse vulnerability, however, has received relatively little attention. Therefore, in the present study, we used an abstinence-based relapse model in rats to test the hypothesis that exposure to chronic stress increases subsequent relapse vulnerability. Rats were trained to press a lever for highly palatable food reinforcers in daily 3-h sessions and then tested for food seeking (i...
November 11, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27845187/basolateral-amygdalar-d2-receptor-activation-is-required-for-the-companions-exerted-suppressive-effect-on-the-cocaine-conditioning
#13
Wen-Yu Tzeng, Chian-Fang G Cherng, Lung Yu, Ching-Yi Wang
The presence of companions renders decreases in cocaine-stimulated dopamine release in the nucleus accumbens and cocaine-induced conditioned place preference (CPP) magnitude. Limbic systems are widely believed to underlie the modulation of accumbal dopamine release and cocaine conditioning. Thus, this study aimed to assess whether intact basolateral nucleus of amygdala (BLA), dorsal hippocampus (DH), and dorsolateral striatum (DLS) is required for the companions-exerted suppressive effect on the cocaine-induced CPP...
November 11, 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/27836941/target-site-investigation-for-the-plasma-prolactin-response-mechanism-based-pharmacokinetic-pharmacodynamic-analysis-of-risperidone-and-paliperidone-in-the-rat
#14
Shinji Shimizu, Sandra M den Hoedt, Victor Mangas Sanjuan, Sinziana Cristea, Jana K Geuer, Dirk-Jan van den Berg, Robin Hartman, Francisco Bellanti, Elizabeth C M de Lange
In order to understand the drivers in the biological system response to dopamine D2 receptor antagonists, a mechanistic semi-physiologically-based (PB) pharmacokinetic-pharmacodymanic (PKPD) model was developed to describe prolactin responses to risperidone (RIS) and its active metabolite paliperidone (PAL). A microdialysis study in rats was performed to obtain detailed plasma, brain extracellular fluid (brainECF), and cerebrospinal fluid (CSF) concentrations of PAL and RIS. To assess the impact of P-gp functioning on brain distribution, experiments were performed in absence or presence of the P-glycoprotein (P-gp) inhibitor tariquidar (TQD)...
November 11, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27834847/astaxanthin-and-docosahexaenoic-acid-reverse-the-toxicity-of-the-maxi-k-bk-channel-antagonist-mycotoxin-penitrem-a
#15
Amira A Goda, Khayria M Naguib, Magdy M Mohamed, Hassan A Amra, Somaia A Nada, Abdel-Rahman B Abdel-Ghaffar, Chris R Gissendanner, Khalid A El Sayed
Penitrem A (PA) is a food mycotoxin produced by several terrestrial and few marine Penicillium species. PA is a potent tremorgen through selective antagonism of the calcium-dependent potassium BK (Maxi-K) channels. Discovery of natural products that can prevent the toxic effects of PA is important for food safety. Astaxanthin (AST) is a marine natural xanthophyll carotenoid with documented antioxidant activity. Unlike other common antioxidants, AST can cross blood brain barriers (BBBs), inducing neuroprotective effects...
November 9, 2016: Marine Drugs
https://www.readbyqxmd.com/read/27834145/pharmacogenetics-and-pharmacotherapy-of-military-personnel-suffering-from-posttraumatic-stress-disorder
#16
Janine Naß, Thomas Efferth
BACKGROUND: Posttraumatic stress disorder (PTSD) is a severe problem among soldiers with combat experience and still difficult to treat. The pathogenesis is still not fully understood at the psychological level. Therefore, genetic research became a focus of interest. The identification of single nucleotide polymorphisms (SNPs) may help to predict, which persons are at high risk to develop PTSD as a starting point to develop novel targeted drugs for treatment. METHODS: We conducted a systematic review on SNPs in genes related to PTSD pathology and development of targeted pharmacological treatment options based on PubMed database searches...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#17
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/27833003/brain-histamine-depletion-enhances-the-behavioural-sequences-complexity-of-mice-tested-in-the-open-field-partial-reversal-effect-of-the-dopamine-d2-d3-antagonist-sulpiride
#18
Andrea Santangelo, Gustavo Provensi, Alessia Costa, Patrizio Blandina, Valdo Ricca, Giuseppe Crescimanno, Maurizio Casarrubea, M Beatrice Passani
Markers of histaminergic dysregulation were found in several neuropsychiatric disorders characterized by repetitive behaviours, thoughts and stereotypies. We analysed the effect of acute histamine depletion by means of i. c.v. injections of alpha-fluoromethylhistidine, a blocker of histidine decarboxylase, on the temporal organization of motor sequences of CD1 mice behaviour in the open-field test. An ethogram encompassing 9 behavioural components was employed. Durations and frequencies were only slightly affected by treatments...
November 8, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27829813/olanzapine-induced-biochemical-and-histopathological-changes-after-its-chronic-administration-in-rats
#19
Rehmat Shah, Fazal Subhan, Gowhar Ali, Ihsan Ullah, Sami Ullah, Muhammad Shahid, Nisar Ahmad, Khwaja Fawad
Objective: Olanzapine is a second generation antipsychotic acting mainly as a dopamine D2 and serotonine 5-HT2 receptors antagonist prescribed in the treatment of schizophrenia and various other psychiatric illnesses. Even though olanzapine is widely used in psychiatry, its effects on the architecture of pancreas, liver and kidneys are little known. The histology of pancreas especially has never been studied. For these reasons, the current study was designed to elucidate the toxic effects of chronic administration of olanzapine on pancreas, liver and kidneys and the enzymes released by these tissues in an escalating dose manner...
November 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/27824052/augmentation-of-heroin-seeking-following-chronic-food-restriction-in-the-rat-differential-role-for-dopamine-transmission-in-the-nucleus-accumbens-shell-and-core
#20
Tracey M D'Cunha, Emilie Daoud, Damaris Rizzo, Audrey Bishop, Melissa Russo, Gabrielle Mourra, Laurie Hamel, Firas Sedki, Uri Shalev
Caloric restriction during drug abstinence increases the risk for relapse in addicts. In rats, chronic food restriction during a period of withdrawal following heroin self-administration augments heroin seeking. The mechanisms underlying this effect are largely unknown. Here, we investigated the role of nucleus accumbens (NAc) shell and core dopamine (DA) in food restriction-induced augmentation of heroin seeking. Rats were trained to self-administer heroin (0.1 mg/kg/infusion) for 10 days. Next, rats were moved to the animal colony for a withdrawal period, during which rats were food restricted to 90% of their original body weight (FDR group) or given unrestricted access to food (sated group)...
November 8, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
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