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https://www.readbyqxmd.com/read/28097374/effects-of-5-ht1a-5-ht2a-and-5-ht2c-receptor-agonists-and-antagonists-on-responding-for-a-conditioned-reinforcer-and-its-enhancement-by-methylphenidate
#1
Paul J Fletcher, Fiona D Zeeb, Caleb J Browne, Guy A Higgins, Ashlie D Soko
OBJECTIVES: These experiments examined the effects of selective 5-HT1A, 5-HT2A and 5-HT2C receptor ligands on responding for a conditioned reinforcer (CRf). Effects of these ligands were measured under basal conditions and following elevated dopamine (DA) activity produced by the DA reuptake inhibitor methylphenidate. METHODS: Water-restricted rats learned to associate a conditioned stimulus (CS) with water in operant chambers. Subsequently, two response levers were made available; responding on one lever delivered the CS (now a CRf), while responding on the second lever had no consequences...
January 18, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28096672/a-biopsychological-review-of-gambling-disorder
#2
REVIEW
Gabriel C Quintero
The present review is an overview of previous experimental work on biopsychological aspects of gambling disorder. It includes the topics 1) gambling disorder from the neuroimaging and electroencephalography (EEG) perspective, 2) cognitive, executive functioning, and neuropsychological aspects of gambling disorder, and 3) rodent models of gambling disorder. Penalties and losses in gambling can differ in terms of brain activity. Also, specific patterns of brain activity, brain anatomical traits, EEG responses, and cognitive and executive performance can discriminate pathological gamblers from nonpathological gamblers...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28095003/cocaine-addiction-as-a-homeostatic-reinforcement-learning-disorder
#3
Mehdi Keramati, Audrey Durand, Paul Girardeau, Boris Gutkin, Serge H Ahmed
Drug addiction implicates both reward learning and homeostatic regulation mechanisms of the brain. This has stimulated 2 partially successful theoretical perspectives on addiction. Many important aspects of addiction, however, remain to be explained within a single, unified framework that integrates the 2 mechanisms. Building upon a recently developed homeostatic reinforcement learning theory, the authors focus on a key transition stage of addiction that is well modeled in animals, escalation of drug use, and propose a computational theory of cocaine addiction where cocaine reinforces behavior due to its rapid homeostatic corrective effect, whereas its chronic use induces slow and long-lasting changes in homeostatic setpoint...
January 16, 2017: Psychological Review
https://www.readbyqxmd.com/read/28092019/urb597-and-the-cannabinoid-win55-212-2-reduce-behavioral-and-neurochemical-deficits-induced-by-mptp-in-mice-possible-role-of-redox-modulation-and-nmda-receptors
#4
Angel Escamilla-Ramírez, Esperanza García, Guadalupe Palencia-Hernández, Ana Laura Colín-González, Sonia Galván-Arzate, Isaac Túnez, Julio Sotelo, Abel Santamaría
Several physiological events in the brain are regulated by the endocannabinoid system (ECS). While synthetic cannabinoid receptor (CBr) agonists such as WIN55,212-2 act directly on CBr, agents like URB597, a fatty acid amide hydrolase (FAAH) inhibitor, induce a more "physiological" activation of CBr by increasing the endogenous levels of the endocannabinoid anandamide (AEA). Herein, we compared the pre- and post-treatment efficacy of URB597 and WIN55,212-2 on different endpoints evaluated in the toxic model produced by the mitochondrial toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in mice...
January 14, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28087732/novel-gnb1-mutations-disrupt-assembly-and-function-of-g-protein-heterotrimers-and-cause-global-developmental-delay-in-humans
#5
Katja Lohmann, Ikuo Masuho, Dipak N Patil, Hauke Baumann, Eva Hebert, Sofia Steinrücke, Daniel Trujillano, Nickolas K Skamangas, Valerija Dobricic, Irina Hüning, Gabriele Gillessen-Kaesbach, Ana Westenberger, Dusanka Savic-Pavicevic, Alexander Münchau, Gabriela Oprea, Christine Klein, Arndt Rolfs, Kirill A Martemyanov
Global developmental delay (GDD), often accompanied by intellectual disability, seizures and other features is a severe, clinically and genetically highly heterogeneous childhood-onset disorder. In cases where genetic causes have been identified, de-novo mutations in neuronally expressed genes are a common scenario. These mutations can be best identified by exome sequencing of parent-offspring trios. De novo mutations in the guanine nucleotide-binding protein, beta 1 (GNB1) gene, encoding the Gβ1 subunit of heterotrimeric G proteins, have recently been identified as a novel genetic cause of GDD...
January 13, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28075189/11-analytically-confirmed-cases-of-mexedrone-use-among-polydrug-users
#6
Liam Roberts, Loretta Ford, Neel Patel, J Allister Vale, Sally M Bradberry
INTRODUCTION: Mexedrone, 3-methoxy-2-(methylamino)-1-(4-methylphenyl)propan-1-one, is the alpha-methoxy-derivative of mephedrone (4-methyl-N-methyl cathinone). Mexedrone inhibits the re-uptake of serotonin and dopamine in a dose-dependent manner and has affinity for serotonin and dopamine membrane transporters and receptors (5-HT2 and D2 receptors), producing sympathomimetic effects similar to amfetamines. To date there are no published clinical reports on mexedrone use that are analytically confirmed...
January 11, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28074831/rgs9-2-modulates-responses-to-oxycodone-in-pain-free-and-chronic-pain-states
#7
Sevasti Gaspari, Valeria Cogliani, Lefteris Manouras, Ethan M Anderson, Vasiliki Mitsi, Kleopatra Avrampou, Fiona B Carr, Venetia Zachariou
Regulator of G protein signalling 9-2 (RGS9-2) is a striatal enriched signal transduction modulator, known to play a critical role in the development of addiction-related behaviours following exposure to psychostimulants or opioids. RGS9-2 controls the function of several GPCRs, including dopamine and mu opioid (MOR) receptors. We previously showed that RGS9-2 complexes negatively control morphine analgesia, and promote the development of morphine tolerance. In contrast, RGS9-2 positively modulates the actions of other opioid analgesics, such as fentanyl and methadone...
January 11, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28069917/dopamine-modulates-the-functional-organization-of-the-orbitofrontal-cortex
#8
Thorsten Kahnt, Philippe N Tobler
: Neuromodulators such as dopamine can alter the intrinsic firing properties of neurons, and may thereby change the configuration of larger functional circuits. The primate orbitofrontal cortex (OFC) receives dopaminergic input from midbrain nuclei, but the role of dopamine in the OFC is still unclear. Here we tested the idea that dopaminergic activity changes the pattern of connectivity between the OFC and the rest of the brain, and thereby reconfigures functional networks in the OFC...
January 9, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28065934/brain-cannabinoid-receptor-2-expression-function-and-modulation
#9
REVIEW
De-Jie Chen, Ming Gao, Fen-Fei Gao, Quan-Xi Su, Jie Wu
Cannabis sativa (marijuana) is a fibrous flowering plant that produces an abundant variety of molecules, some with psychoactive effects. At least 4% of the world's adult population uses cannabis annually, making it one of the most frequently used illicit drugs in the world. The psychoactive effects of cannabis are mediated primarily through cannabinoid receptor (CBR) subtypes. The prevailing view is that CB1Rs are mainly expressed in the central neurons, whereas CB2Rs are predominantly expressed in peripheral immune cells...
January 9, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28063918/simultaneous-in-vivo-receptor-occupancy-assays-for-serotonin-1a-2a-and-dopamine-2-receptors-with-the-use-of-non-radiolabelled-tracers-proposed-method-in-screening-antipsychotics
#10
Jagadeesh Babu Thentu, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Devender Reddy Ajjala, Raghupathi Reddy Aleti, Veera Raghava Choudary Palacharla
INTRODUCTION: Conventionally, receptor occupancy assays employ radiolabelled tracer.However, recent advances with non-radiolabelled tracers brought a revolution in target engagement assays.Non-radiolabelled tracer based receptor occupancy uses LC-MS/MS based quantification.It offers simultaneous quantification of more than one tracer; thus, provides the feasibility of evaluating multiple targets in a single animal.In the present study, we demonstrated simultaneous measurement of serotonin 1A, serotonin 2A, and dopamine 2 receptor occupancy using non-radiolabelled tracers in rats...
January 4, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28059046/long-term-effects-of-aripiprazole-exposure-on-monoaminergic-and-glutamatergic-receptor-subtypes-comparison-with-cariprazine
#11
Yong Kee Choi, Nika Adham, Béla Kiss, István Gyertyán, Frank I Tarazi
OBJECTIVE: This study examined the chronic effects of aripiprazole and cariprazine on serotonin (5-HT1A and 5-HT2A) and glutamate (NMDA and AMPA) receptor subtypes. In addition, the effects of aripiprazole on D2 and D3 receptors were tested and compared with previously reported cariprazine data. METHODS: Rats received vehicle, aripiprazole (2, 5, or 15 mg/kg), or cariprazine (0.06, 0.2, or 0.6 mg/kg) for 28 days. Receptor levels were quantified using autoradiographic assays on brain sections from the medial prefrontal cortex (MPC), dorsolateral frontal cortex (DFC), nucleus accumbens (NAc), caudate-putamen medial (CPu-M), caudate-putamen lateral (CPu-L), hippocampal CA1 (HIPP-CA1) and CA3 (HIPP-CA3) regions, and the entorhinal cortex (EC)...
January 6, 2017: CNS Spectrums
https://www.readbyqxmd.com/read/28057528/role-of-d2-dopamine-receptors-of-the-ventral-pallidum-in-inhibitory-avoidance-learning
#12
László Lénárd, Tamás Ollmann, Kristóf László, Anita Kovács, Rita Gálosi, Veronika Kállai, Tóth Attila, Erika Kertes, Olga Zagoracz, Zoltán Karádi, László Péczely
In our present experiments, the role of D2 dopamine (DA) receptors of the ventral pallidum (VP) was investigated in one trial step-through inhibitory avoidance paradigm. Animals were shocked 3 times in the conditioning trial, with 0.5mA current for 1s. Subsequently bilateral microinjection of the D2 DA receptor agonist quinpirole was administered into the VP in three doses (0.1μg, 1.0μg or 5.0μg in 0.4μl saline). We also applied the D2 DA receptor antagonist sulpiride (0.4μg in 0.4μl saline) alone or 15min prior to the agonist treatment to elucidate whether the agonist effect was specific for the D2 DA receptors...
January 3, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28044942/emerging-pharmacological-therapies-in-schizophrenia-what-s-new-what-s-different-what-s-next
#13
Leslie Citrome
There are several new and emerging medication interventions for both the acute and maintenance treatment phases of schizophrenia. Recently approved are 2 new dopamine receptor partial agonists, brexpiprazole and cariprazine, as well as 2 new long-acting injectable antipsychotic formulations, aripiprazole lauroxil and 3-month paliperidone palmitate. Although differences in efficacy compared to other available choices are not expected, the new oral options offer different tolerability profiles that may be attractive for individual patients who have had difficulties with older medications...
December 2016: CNS Spectrums
https://www.readbyqxmd.com/read/28041915/identification-of-multi-targeted-anti-migraine-potential-of-nystatin-and-development-of-its-brain-targeted-chitosan-nanoformulation
#14
Priti Girotra, Aman Thakur, Ajay Kumar, Shailendra Kumar Singh
The complex pathophysiology involved in migraine necessitates the drug treatment to act on several receptors simultaneously. The present investigation was an attempt to discover the unidentified anti-migraine activity of the already marketed drugs. Shared featured pharmacophore modeling was employed for this purpose on six target receptors (β2 adrenoceptor, Dopamine D3, 5HT1B, TRPV1, iGluR5 kainate and CGRP), resulting in the generation of five shared featured pharmacophores, which were further subjected to virtual screening of the ligands obtained from Drugbank database...
December 29, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28038309/diazepam-inhibits-electrically-evoked-and-tonic-dopamine-release-in-the-nucleus-accumbens-and-reverses-the-effect-of-amphetamine
#15
Alexander Gomez-A, Amanda Maino Fiorenza, Suelen Lucio Boschen, Adam H Sugi, Danielle Beckman, Sergio T Ferreira, Kendall H Lee, Charles D Blaha, Claudio Da Cunha
Diazepam is a benzodiazepine receptor agonist with anxiolytic and addictive properties. Although most drugs of abuse increase dopamine release in the nucleus accumbens, here we show that not only it causes the opposite effect but also prevents amphetamine action on increasing dopamine release. We used 20 min sampling in vivo microdialysis and subsecond fast-scan cyclic voltammetry recordings at carbon-fiber microelectrodes to show that diazepam caused a dose-dependent decrease in tonic and electrically-evoked dopamine release in the nucleus accumbens of urethane anesthetized adult male Swiss mice...
December 30, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28034961/role-of-prefrontal-serotonergic-and-dopaminergic-systems-in-encounter-induced-hyperactivity-in-methamphetamine-sensitized-mice
#16
Tatsunori Tanaka, Yukio Ago, Chiaki Umehara, Emina Imoto, Shigeru Hasebe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsuda
BACKGROUND: Isolation-reared mice show social encounter-induced hyperactivity with activation of prefrontal serotonergic and dopaminergic systems, but it is not known whether this stress response is observed in other pathological conditions. Here we examined whether the social encounter stimulation induces abnormal behavior during withdrawal in chronic methamphetamine (METH)-treated mice. METHODS: To induce METH-induced behavioral sensitization, male mice were injected with METH (1 mg/kg) once daily for 7 days...
December 29, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28032125/effects-of-dopamine-d1-and-d2-receptor-agonists-on-environmental-enrichment-attenuated-sucrose-cue-reactivity-in-rats
#17
Edwin Glueck, Darren Ginder, Jeff Hyde, Katherine North, Jeffrey W Grimm
RATIONALE: Acute or chronic environmental enrichment (EE) reduces sucrose cue reactivity in rats. This effect may be mediated by dopamine receptors. OBJECTIVES: We examined whether dopamine D1 or D2 receptor agonism could reverse the EE effect. We also examined whether any reversal effects would vary with the incubation of sucrose craving. METHODS: Following 10 days (2 h/day) of sucrose self-administration, rats experienced either 1 or 30 days of forced abstinence and either overnight (acute) or 29 day (chronic) EE...
December 28, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/28026009/transcriptomic-profiling-of-platelet-senescence-and-platelet-extracellular-vesicles
#18
Annika Pienimaeki-Roemer, Tatiana Konovalova, Melina M Musri, Alexander Sigruener, Alfred Boettcher, Gunter Meister, Gerd Schmitz
BACKGROUND: Platelets (PLTs) are derived from megakaryocytes during PLT shedding. Senescent or activated PLTs are expanded in vascular and neurological diseases and release PLT extracellular vesicles (PL-EVs). A systematic analysis of regular messenger RNA (mRNA) and small RNA composition in PLTs and PL-EVs during in vitro PLT senescence has not yet been published. STUDY DESIGN AND METHODS: We isolated PLTs, total PL-EVs, and PL-EV subsets on Days 0 and 5 from human stored donor platelet concentrates...
January 2017: Transfusion
https://www.readbyqxmd.com/read/28018211/cistanche-tubulosa-protects-dopaminergic-neurons-through-regulation-of-apoptosis-and-glial-cell-derived-neurotrophic-factor-in-vivo-and-in-vitro
#19
Qian Xu, Wen Fan, Shui-Fen Ye, Yi-Bo Cong, Wei Qin, Shi-Ya Chen, Jing Cai
Parkinson's disease (PD) is a neurodegenerative disease with the pathological hallmark of reduced nigrostriatal dopamine. In traditional Chinese medicine (TCM) clinical practice, the nanopowder of Cistanche tubulosa has therapeutic effects on PD. To identify the therapeutic mechanism, this study tested the protective effect of different doses of MPP(+)-induced toxicity in MES23.5 cells using the MTT assay and in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD mice (vehicles). Immunohistochemistry was used to assess cytomorphology and tyrosine hydroxylase (TH) expression...
2016: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28013351/differential-effects-of-aprepitant-a-clinically-used-neurokinin-1-receptor-antagonist-on-the-expression-of-conditioned-psychostimulant-versus-opioid-reward
#20
Padmanabhan Mannangatti, Santhanalakshmi Sundaramurthy, Sammanda Ramamoorthy, Lankupalle D Jayanthi
RATIONALE: Neurokinin-1 receptor (NK1R) signaling modulates behaviors associated with psychostimulants and opioids. Psychostimulants, such as amphetamine (AMPH) and cocaine, bind to monoamine transporters and alter their functions. Both dopamine and norepinephrine transporters are regulated by NK1R activation suggesting a role for NK1R mediated catecholamine transporter regulation in psychostimulant-mediated behaviors. OBJECTIVES: The effect of in vivo administration of aprepitant (10 mg/kg) on the expression of AMPH (0...
December 24, 2016: Psychopharmacology
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