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Dopamine receptor 2

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https://www.readbyqxmd.com/read/29782864/are-dopamine-receptor-and-transporter-changes-in-rett-syndrome-reflected-in-mecp2-deficient-mice
#1
Dean F Wong, Mary E Blue, James R Brašić, Ayon Nandi, Heather Valentine, Kirstie H Stansfield, Olivier Rousset, Genila Bibat, Mary E Yablonski, Michael V Johnston, Albert Gjedde, SakkuBai Naidu
In the present study we tested the claim that the dopaminergic dysfunction of Rett Syndrome (RTT) also occurs in Mecp2-deficient mice that serve as a model of the syndrome. We used positron emission tomography (PET) to image dopamine D2 receptors (D2 R) and transporters (DAT) in women with RTT and in Mecp2-deficient mice, and D1 R and D2 R density was measured in postmortem human tissue by autoradiography. Results showed 1) significantly reduced D2 R density in the striatum of women with RTT compared to control subjects...
May 18, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29781347/interaction-of-drd4-methylation-and-phthalate-metabolites-affects-continuous-performance-test-performance-in-adhd
#2
Johanna Inhyang Kim, Jae-Won Kim, Inkyung Shin, Bung-Nyun Kim
OBJECTIVE: We investigated the interaction effect between the methylation of dopamine receptor D4 (DRD4) and phthalate exposure in ADHD on continuous performance test (CPT) variables. METHOD: Urine concentrations of mono-(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP), mono-(2-ethyl-5-oxohexyl) phthalate (MEOHP), and mono-n-butyl phthalate (MBP) were tested. The methylation status was analyzed for CpG sites of DRD4. Multivariable linear regression models were applied to investigate the interaction effects of methylation and phthalate levels...
May 1, 2018: Journal of Attention Disorders
https://www.readbyqxmd.com/read/29779874/a-gabaergic-feedback-shapes-dopaminergic-input-on-the-drosophila-mushroom-body-to-promote-appetitive-long-term-memory
#3
Alice Pavlowsky, Johann Schor, Pierre-Yves Plaçais, Thomas Preat
Memory consolidation is a crucial step for long-term memory (LTM) storage. However, we still lack a clear picture of how memory consolidation is regulated at the neuronal circuit level. Here, we took advantage of the well-described anatomy of the Drosophila olfactory memory center, the mushroom body (MB), to address this question in the context of appetitive LTM. The MB lobes, which are made by the fascicled axons of the MB intrinsic neurons, are organized into discrete anatomical modules, each covered by the terminals of a defined type of dopaminergic neuron (DAN) and the dendrites of a corresponding type of MB output neuron (MBON)...
May 9, 2018: Current Biology: CB
https://www.readbyqxmd.com/read/29775777/antidepressant-potential-of-novel-flavonoids-derivatives-from-sweet-violet-viola-odorata-l-pharmacological-biochemical-and-computational-evidences-for-possible-involvement-of-serotonergic-mechanism
#4
Nasiara Karim, Imran Khan, Abeer Abdelhalim, Ajmal Khan, Sobia Ahsan Halim
Plant-derived natural constituents are of great interest in modern drug discovery due to their natural diversity. Viola odorata L has been traditionally used for the treatment of neuropsychiatric disorders. The present study was undertaken to isolate phytoconstituents including three flavonoids 5,7-Dihydroxy-3,6-dimethoxyflavone[1] 5,7,4'-trihydroxy-3',5'dimethoxyflavone [2] and 5,7,4'-trihydroxy-3'-methoxyflavone [3] from the whole plant of Viola odorata L and to investigate the antidepressant-like effects of these compounds and their possible mechanism of action using antagonists of the serotonergic, dopaminergic and adrenergic system...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29775630/the-basolateral-amygdala-dopaminergic-system-contributes-to-the-improving-effect-of-nicotine-on-stress-induced-memory-impairment-in-rats
#5
Elnaz Keshavarzian, Zahra Ghasemzadeh, Ameneh Rezayof
Stress seems to be an important risk factor in the beginning and continuing stages of cigarette tobacco smoking in humans. Considering that both of nicotine administration and stress exposure affect cognitive functions including memory formation, the aim of the present study was 1) to evaluate the effect of subcutaneous (s.c.) administration of nicotine on memory formation under stress and 2) to assess the possible role of the basolateral amygdala (BLA) dopamine D1 and D2 receptors in the effect of nicotine on stress-induced memory retrieval impairment...
May 15, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29773910/the-l-type-calcium-channel-blocker-isradipine-attenuates-cue-induced-cocaine-seeking-by-enhancing-dopaminergic-activity-in-the-ventral-tegmental-area-to-nucleus-accumbens-pathway
#6
Nii A Addy, Eric J Nunes, Shannon M Hughley, Keri M Small, Sarah J Baracz, Joshua L Haight, Anjali M Rajadhyaksha
Previous preclinical and clinical investigations have focused on the L-type calcium channel (LTCC) as a potential therapeutic target for substance abuse. While some clinical studies have examined the ability of LTCC blockers to alter cocaine's subjective effects, very few LTCC studies have examined cocaine relapse. Here, we examined whether ventral tegmental area (VTA)-specific or systemic administration of the LTCC inhibitor, isradipine, altered cocaine-seeking behavior in a rat model. Male Sprague-Dawley rats first received 10 days of cocaine self-administration training (2 h sessions), where active lever depression resulted in delivery of a ∼0...
May 3, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29773888/antitumor-effect-of-axitinib-combined-with-dopamine-and-pk-pd-modeling-in-the-treatment-of-human-breast-cancer-xenograft
#7
Yuan-Heng Ma, Si-Yuan Wang, Yu-Peng Ren, Jian Li, Ting-Jie Guo, Wei Lu, Tian-Yan Zhou
Rising evidence has shown the development of resistance to vascular endothelial growth factor receptor (VEGFR) inhibitors in the practices of cancer therapy. It is reported that the efficacy of axitinib (AX), a VEGFR inhibitor, is limited in the treatment of breast cancer as a single agent or in combination with other chemotherapeutic drugs due to the probability of rising population of cancer stem-like cells (CSCs) caused by AX. The present study evaluated the effect of dopamine (DA) improving AX's efficacy on MCF-7/ADR breast cancer in vitro and in vivo, and developed a pharmacokinetic-pharmacodynamic (PK-PD) model describing the in vivo experimental data and characterizing the interaction of effect between AX and DA...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29772491/calpain-inhibition-reduces-nmda-receptor-rundown-in-rat-substantia-nigra-dopamine-neurons
#8
Jerry Zhao, Michel Baudry, Susan Jones
Repeated activation of N-Methyl-d-aspartate receptors (NMDARs) causes a Ca2+ -dependent reduction in NMDAR-mediated current in dopamine (DA) neurons of the substantia nigra pars compacta (SNc) in one week old rats; however, a Ca2+ -dependent regulatory protein has not been identified. The role of the Ca2+ -dependent cysteine protease, calpain, in mediating NMDAR current rundown was investigated. In brain slices from rats aged postnatal day 7-9 ('P7'), bath application of either of the membrane permeable calpain inhibitors, N-Acetyl-L-leucyl-L-leucyl-L-norleucinal (ALLN, 20 μM) or MDL-28170 (30 μM) significantly reduced whole-cell NMDAR current rundown...
May 4, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29770746/-express-chronic-inflammatory-pain-decreases-the-glutamate-vesicles-in-presynaptic-terminals-of-the-nucleus-accumbens
#9
Chuchu Qi, Baolin Guo, Keke Ren, Han Yao, Mengmeng Wang, Tangna Sun, Guohong Cai, Haiying Liu, Rui Li, Ceng Luo, Wenting Wang, Sheng-Xi Wu
Reward system has been proved to be important to nociceptive behavior, and the nucleus accumbens (NAc) is a key node in reward circuitry. It has been further revealed that dopamine system modulates the NAc to influence the pain sensation, whereas the role of glutamatergic projection in the NAc in the modulation of chronic pain is still elusive. In this study, we used a Complete Freund adjuvant (CFA) -induced chronic inflammatory pain model to explore the changes of the glutamatergic terminals in the NAc, and we found that following the chronic inflammation, the protein level of vesicular glutamate transporters1 (VGLUT1) was significant decreased in the NAc...
January 1, 2018: Molecular Pain
https://www.readbyqxmd.com/read/29767374/the-effect-of-ca1-dopaminergic-system-on-amnesia-induced-by-harmane-in-mice
#10
Mohammad Nasehi, Simin Hasanvand, Fatemeh Khakpai, Mohammad-Reza Zarrindast
In the present study, the effects of bilateral injections of dopaminergic drugs into the hippocampal CA1 regions (intra-CA1) on harmane-induced amnesia were examined in mice. We used a single-trial step-down inhibitory avoidance task for the assessment of memory acquisition in adult male mice. Our data indicated that pre-training intra-peritoneal (i.p.) administration of harmane (12 mg/kg) impaired memory acquisition. Moreover, intra-CA1 administration of dopamine D1 receptor agonist, SKF38393 (0.25 µg/mouse), dopamine D1 receptor antagonist, SCH23390 (0...
May 16, 2018: Acta Neurologica Belgica
https://www.readbyqxmd.com/read/29748774/structural-determinants-influencing-halogen-bonding-a-case-study-on-azinesulfonamide-analogs-of-aripiprazole-as-5-ht-1a-5-ht-7-and-d-2-receptor-ligands
#11
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J Bojarski, Joachim Kusz, Paweł Zajdel
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated. In vitro methods are used to determine their affinity for serotonin 5-HT1A , 5-HT6 , 5-HT7 , and dopamine D2 receptors. X-ray analysis, two-dimensional NMR conformational studies, and docking into the 5-HT1A and 5-HT7 receptor models are then conducted to investigate the conformational preferences of selected serotonin receptor ligands in different environments...
May 11, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29730036/the-effects-of-fathering-experience-on-paternal-behaviors-and-levels-of-central-expression-of-oxytocin-and-dopamine-2-type-receptors-in-mandarin-voles
#12
Bo Wang, Lu Wang, Kai Wang, Fadao Tai
Mothers' brains change dramatically in response to the release of hormones related to pregnancy and labor; however, fathers' brains are also sensitive to the experience of paternal care. Thus, fathers with differing fathering experience may exhibit different behavioral responses towards pups. Using socially monogamous mandarin voles (Microtus mandarinus), effects of fathering experience on levels of paternal behavior as well as oxytocin (OT) and dopamine-2 type (D2) receptors in the nucleus accumbens (NaCC) and medial nucleus of the amygdala (MeA) were investigated...
May 2, 2018: Physiology & Behavior
https://www.readbyqxmd.com/read/29729893/memantine-ameliorates-depressive-like-behaviors-by-regulating-hippocampal-cell-proliferation-and-neuroprotection-in-olfactory-bulbectomized-mice
#13
Kohei Takahashi, Osamu Nakagawasai, Wataru Nemoto, Shogo Kadota, Jinichi Isono, Takayo Odaira, Wakana Sakuma, Yuichiro Arai, Takeshi Tadano, Koichi Tan-No
Our previous study suggested that the non-competitive N-methyl-d-aspartate receptor antagonist memantine (MEM) inhibits dopamine (DA) reuptake and turnover by inhibiting brain monoamine oxidase. Clinical studies have reported that MEM may improve depressive symptoms; however, specific mechanisms underlying this effect are unclear. We performed emotional behavior, tail suspension, and forced swimming tests to examine whether MEM has antidepressant effects in olfactory bulbectomized (OBX) mice, an animal model of depression...
May 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29729086/the-novel-atypical-antipsychotic-cariprazine-demonstrates-dopamine-d-2-receptor-dependent-partial-agonist-actions-on-rat-mesencephalic-dopamine-neuronal-activity
#14
Sarah Delcourte, Charles R Ashby, Renaud Rovera, Béla Kiss, Nika Adham, Bence Farkas, Nasser Haddjeri
AIM: Cariprazine, a dopamine D3 -preferring D3 /D2 receptor partial agonist, is FDA approved for the treatment of schizophrenia and acute manic or mixed episodes of bipolar disorder. This study used in vivo electrophysiological techniques in anesthetized rats to determine cariprazine's effect on dopaminergic cell activity in the ventral tegmental area (VTA) and substantia nigra pars compacta (SNc). METHODS: Extracellular recordings of individual dopaminergic neurons were performed after oral or intravenous administration of cariprazine, the D3 receptor antagonist SB 277011A, the D2 receptor antagonist L741,626, and/or the D3 receptor agonist PD 128,907...
May 4, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29726995/the-balance-of-pi3k-and-erk-signaling-is-dysregulated-in-prolactinoma-and-modulated-by-dopamine
#15
Allyson K Roof, Siwanon Jirawatnotai, Tammy Trudeau, Crystal Kuzyk, Margaret E Wierman, Hiroaki Kiyokawa, Arthur Gutierrez-Hartmann
Prolactin-secreting adenomas, or prolactinomas, cause hypogonadism, osteoporosis, and infertility. Although dopamine agonists (DAs) are used clinically to treat prolactinoma, and reduce prolactin secretion via cAMP inhibition, the precise mechanism by which DAs inhibit lactotrope proliferation has not been defined. Here we report the novel finding that PI3K signals through AKT and mTOR to drive proliferation of pituitary somatolactotrope GH4T2 cells. We demonstrate that the DA cabergoline reduces activity of the mTOR effector s6K, and diminishes GH4T2 cell proliferation primarily via activation of the long isoform of the dopamine D2 receptor (D2R)...
May 2, 2018: Endocrinology
https://www.readbyqxmd.com/read/29725947/individual-differences-in-dopamine-d-2-receptor-availability-correlate-with-reward-valuation
#16
Linh C Dang, Gregory R Samanez-Larkin, Jaime J Castrellon, Scott F Perkins, Ronald L Cowan, David H Zald
Reward valuation, which underlies all value-based decision-making, has been associated with dopamine function in many studies of nonhuman animals, but there is relatively less direct evidence for an association in humans. Here, we measured dopamine D2 receptor (DRD2) availability in vivo in humans to examine relations between individual differences in dopamine receptor availability and neural activity associated with a measure of reward valuation, expected value (i.e., the product of reward magnitude and the probability of obtaining the reward)...
May 3, 2018: Cognitive, Affective & Behavioral Neuroscience
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#17
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29722299/the-adjustment-of-%C3%AE-aminobutyric-acid-a-tonic-subunits-in-huntington-s-disease-from-transcription-to-translation-to-synaptic-levels-into-the-neostriatum
#18
REVIEW
Abraham Rosas-Arellano, Argel Estrada-Mondragón, Carola A Mantellero, Carlos Tejeda-Guzmán, Maite A Castro
γ-Aminobutyric acid (GABA), plays a key role in all stages of life, also is considered the main inhibitory neurotransmitter. GABA activates two kind of membrane receptors known as GABAA and GABAB , the first one is responsible to render tonic inhibition by pentameric receptors containing α4-6, β3, δ, or ρ1-3 subunits, they are located at perisynaptic and/or in extrasynaptic regions. The biophysical properties of GABAA tonic inhibition have been related with cellular protection against excitotoxic injury and cell death in presence of excessive excitation...
April 2018: Neural Regeneration Research
https://www.readbyqxmd.com/read/29717334/the-role-of-striatal-dopamine-d-2-3-receptors-in-cognitive-performance-in-drug-free-patients-with-schizophrenia
#19
Tanja Veselinović, Ingo Vernaleken, Hildegard Janouschek, Paul Cumming, Michael Paulzen, Felix M Mottaghy, Gerhard Gründer
OBJECTIVE: A considerable body of research links cognitive function to dopaminergic transmission in the prefrontal cortex, but less is known about cognition in relation to striatal dopamine D2/3 receptors in unmedicated patients with psychosis. METHODS: We investigated this association by obtaining PET recordings with the high-affinity D2/3 antagonist ligand [18 F] fallypride in 15 medication-free patients with schizophrenia and 11 healthy controls. On the day of PET scanning, we undertook comprehensive neuropsychological testing and assessment of psychopathology using the Positive and Negative Syndrome Scale (PANSS)...
May 1, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29713785/regulation-of-somatostatin-receptor-2-in-the-context-of-antidepressant-treatment-response-in-chronic-mild-stress-in-rat
#20
Agata Faron-Górecka, Maciej Kuśmider, Joanna Solich, Magdalena Kolasa, Paulina Pabian, Piotr Gruca, Irena Romańska, Dariusz Żurawek, Marta Szlachta, Mariusz Papp, Lucyna Antkiewicz-Michaluk, Marta Dziedzicka-Wasylewska
RATIONALE: The role of somatostatin and its receptors for the stress-related neuropsychiatric disorders has been widely raised. Recently, we have also demonstrated the involvement of somatostatin receptor type 2-sst2R and dopamine receptor type 2-D2R in stress. OBJECTIVE: In this context, we decided to find if these receptors are involved in response to antidepressant treatment in animal model of depression-chronic mild stress (CMS). METHODS: Here, we report data obtained following 7-week CMS procedure...
April 30, 2018: Psychopharmacology
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