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dopamine 2 receptor

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https://www.readbyqxmd.com/read/28820571/comparison-of-spreading-depolarizations-in-the-motor-cortex-and-nucleus-accumbens-similar-patterns-of-oxygen-responses-and-the-role-of-dopamine
#1
Caddy Noahl Hobbs, Gordon Holzberg, Akira S Min, R Mark Wightman
Spreading depolarizations (SD) are pathophysiological phenomena that spontaneously arise in traumatized neural tissue and can promote cellular death. Most investigations of SD are performed in the cortex, a brain region that is susceptible to these depolarizing waves and accessible via a variety of monitoring techniques. Here, we describe SD responses in the cortex and the deep brain region of the nucleus accumbens (NAc) of the anesthetized rat with a minimally invasive, implantable sensor. With high temporal resolution, we characterize the time course of oxygen responses to SD in relation to the electrophysiological depolarization signal...
August 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28816835/acute-worsening-of-tics-on-varenicline
#2
Shivam Om Mittal, Bryan T Klassen, Anhar Hassan, James H Bower, Elizabeth A Coon
OBJECTIVE: The aim of this study was to report worsening of Tourette syndrome (TS) in 2 patients treated with varenicline. BACKGROUND: Abnormal dopaminergic signaling is likely involved in the pathophysiology of TS. Varenicline is a partial α4β2 nicotinic acetylcholine agonist that enhances dopamine release. Therefore, the use of varenicline may influence tics in patients with TS. METHOD: We analyzed and described 2 case studies on patients with significant worsening of tics after treatment with varenicline...
August 14, 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28814122/flibanserin-toxicity-in-a-toddler-following-ingestion
#3
Nicholas Granzella, Betty C Chen, Geoffrey S Baird, Matthew Valento
INTRODUCTION: Flibanserin is a medication recently approved by the FDA for treatment of generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Its mechanism of action is not fully understood but is thought to modulate serotonin receptors and increase levels of norepinephrine and dopamine. While much is known about toxicity of other drugs which affect these systems, there is little information about toxicity of flibanserin at this time. CASE: We present a case of a 2-year-old boy who ingested an estimated 600 mg of his mother's flibanserin...
August 17, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28812124/clozapine-chlorpromazine-and-risperidone-dose-dependently-reduce-emotional-hyperthermia-a-biological-marker-of-salience
#4
William W Blessing, Esther M Blessing, Mazher Mohammed, Youichirou Ootsuka
RATIONALE: We recently introduced a new rat model of emotional hyperthermia in which a salient stimulus activates brown adipose tissue (BAT) thermogenesis and tail artery constriction. Antipsychotic drugs, both classical and second generation, act to reduce excessive assignment of salience to objects and events in the external environment. The close association between salient occurrences and increases in body temperature suggests that antipsychotic drugs may also reduce emotional hyperthermia...
August 15, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28807678/metformin-lowers-%C3%AE-synuclein-phosphorylation-and-upregulates-neurotrophic-factor-in-the-mptp-mouse-model-of-parkinson-s-disease
#5
Nikita Katila, Sunil Bhurtel, Sina Shadfar, Sunil Srivastav, Sabita Neupane, Uttam Ojha, Gil-Saeng Jeong, Dong-Young Choi
In spite of the massive research for the identification of neurorestorative or neuroprotective intervention for curing Parkinson's disease (PD), there is still lack of clinically proven neuroprotective agents. Metformin, a common anti-hyperglycemic drug has been known to possess neuroprotective properties. However, specific mechanisms by which metformin protects neurons from 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) neurotoxicity remain to be elucidated. In this study, we assessed the neuroprotective effects of metformin in the subchronic MPTP model of PD, and explored its feasible mechanisms for neuroprotection...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28807673/gpr55-a-therapeutic-target-for-parkinson-s-disease
#6
Marta Celorrio, Estefanía Rojo-Bustamante, Diana Fernández-Suárez, Elena Sáez, Ander Estella-Hermoso de Mendoza, Christa E Müller, María J Ramírez, Julen Oyarzábal, Rafael Franco, María S Aymerich
The GPR55 receptor is expressed abundantly in the brain, especially in the striatum, suggesting it might fulfill a role in motor function. Indeed, motor behavior is impaired in mice lacking GPR55, which also display dampened inflammatory responses. Abnormal-cannabidiol (Abn-CBD), a synthetic cannabidiol (CBD) isomer, is a GPR55 agonist that may serve as a therapeutic agent in the treatment of inflammatory diseases. In this study, we explored whether modulating GPR55 could also represent a therapeutic approach for the treatment of Parkinson's disease (PD)...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28801916/adenosine-and-dopamine-oppositely-modulate-a-hyperpolarization-activated-current-ih-in-chemosensory-neurons-of-the-rat-carotid-body-in-co-culture
#7
Min Zhang, Cathy Vollmer, Colin A Nurse
Adenosine and dopamine (DA) act as neurotransmitters or neuromodulators at the carotid body (CB) chemosensory synapse, however, their mechanisms of action are not fully understood. Using a functional co-culture model of rat CB chemoreceptor (type I) cell clusters and juxtaposed afferent petrosal neurons (PNs), we tested the hypothesis that adenosine and DA act postsynaptically to modulate a hyperpolarization-activated, cyclic nucleotide-gated (HCN) cation current (Ih ). In whole-cell recordings from hypoxia-responsive PNs, cAMP mimetics enhanced Ih whereas the HCN blocker ZD7288 (2 μm) reversibly inhibited Ih ...
August 12, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28801850/amisulpride-in-the-prevention-of-nausea-and-vomiting-induced-by-cisplatin-based-chemotherapy-a-dose-escalation-study
#8
Jørn Herrstedt, Yvonne Summers, Gedske Daugaard, Thomas B Christensen, Karin Holmskov, Paul D Taylor, Gabriel M Fox, Alexander Molassiotis
PURPOSE: The purpose of this study was to investigate the antiemetic effect of the dopamine D2- and dopamine D3-receptor antagonist, amisulpride, in patients receiving cisplatin-based chemotherapy. METHODS: This dose-finding, non-comparative study investigated the antiemetic effect and safety of increasing doses (2.5, 7.5 and 20 mg) of amisulpride against acute nausea and vomiting in the period 0-24 h after initiation of cisplatin-based chemotherapy. The 20 mg dose was also investigated in combination with the 5-HT3-receptor antagonist, ondansetron...
August 11, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28795276/topiramate-via-nmda-ampa-kainate-gabaa-and-alpha2-receptors-and-by-modulation-of-creb-bdnf-and-akt-gsk3-signaling-pathway-exerts-neuroprotective-effects-against-methylphenidate-induced-neurotoxicity-in-rats
#9
Majid Motaghinejad, Manijeh Motevalian, Sulail Fatima, Tabassom Beiranvand, Shiva Mozaffari
Chronic abuse of methylphenidate (MPH) often causes neuronal cell death. Topiramate (TPM) carries neuroprotective effects, but its exact mechanism of action remains unclear. In the present study, the role of various doses of TPM and its possible mechanisms, receptors and signaling pathways involved against MPH-induced hippocampal neurodegeneration were evaluated in vivo. Thus, domoic acid (DOM) was used as AMPA/kainate receptor agonist, bicuculline (BIC) as GABAA receptor antagonist, ketamine (KET) as NMDA receptor antagonist, yohimbine (YOH) as α2 adrenergic receptor antagonist and haloperidol (HAL) was used as dopamine D2 receptor antagonist...
August 9, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28794174/maternal-western-diet-age-specifically-alters-female-offspring-voluntary-physical-activity-and-dopamine-and-leptin-related-gene-expression
#10
Gregory N Ruegsegger, Kolter B Grigsby, Taylor J Kelty, Terese M Zidon, Thomas E Childs, Victoria J Vieira-Potter, David L Klinkebiel, Michael Matheny, Phillip J Scarpace, Frank W Booth
Prenatal overnutrition affects development into adulthood and influences risk of obesity. We assessed the transgenerational effect of maternal Western diet (WD) consumption on offspring physical activity. Voluntary wheel running was increased in juvenile (4-7 wk of age), but decreased in adult (16-19 wk of age), F1 female WD offspring In contrast, no wheel-running differences in F1 male offspring were observed. Increased wheel running in juvenile female WD offspring was associated with up-regulated dopamine receptor (DRD)-1 and -2 in the nucleus accumbens (NAc) and with down-regulated Lepr in the ventral tegmental area (VTA)...
August 9, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28790021/deficient-striatal-adaptation-in-aminergic-and-glutamatergic-neurotransmission-is-associated-with-tardive-dyskinesia-in-non-human-primates-exposed-to-antipsychotic-drugs
#11
Catherine Lévesque, Giovanni Hernandez, Souha Mahmoudi, Frédéric Calon, Fabrizio Gasparini, Baltazar Gomez-Mancilla, Pierre J Blanchet, Daniel Lévesque
Tardive dyskinesia (TD) is a potentially disabling condition encompassing all delayed, persistent, and often irreversible abnormal involuntary movements arising in a fraction of subjects during long-term exposure to centrally acting dopamine receptor-blocking agents such as antipsychotic drugs and metoclopramide. However, the pathogenesis of TD has proved complex and remains elusive. To investigate the mechanism underlying the development of TD, we have chronically exposed 17 Cebus apella monkeys to typical (11) or atypical (6) antipsychotic drugs...
August 5, 2017: Neuroscience
https://www.readbyqxmd.com/read/28774576/synthesis-and-biological-investigation-of-tetrahydropyridopyrimidinone-derivatives-as-potential-multireceptor-atypical-antipsychotics
#12
Hainimu Xiamuxi, Zhen Wang, Jianfeng Li, Yu Wang, Chunhui Wu, Feipu Yang, Xiangrui Jiang, Yongjian Liu, Qingjie Zhao, Weiming Chen, Jian Zhang, Yuanchao Xie, Tianwen Hu, Mingshuo Xu, Shuang Guo, Haji Akber Aisa, Yang He, Jingshan Shen
In the present study, a series of tetrahydropyridopyrimidinone derivatives, possessing potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (10d) held the best pharmacological profile. It not only exhibited potent and balanced activities for D2, 5-HT1A, and 5-HT2A receptors, but was also endowed with low activities for α1A, 5-HT2C, H1 receptors and hERG channels, suggesting a low propensity for inducing orthostatic hypotension, weight gain and QT prolongation...
July 24, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28774501/synaptic-vesicle-2c-and-its-synaptic-related-function
#13
REVIEW
Yan-Wei Hu, Lei Xiao, Lei Zheng, Qian Wang
Synaptic vesicle 2 C (SV2C) is a novel isoform belonging to the synaptic vesicle 2 (SV2) protein superfamily; a family of proteins known to have roles in vesicle trafficking, exocytosis and neurotransmission. In humans, SV2C is expressed in evolutionarily older brain regions, and is a known receptor for botulinum neurotoxin/A (BoNT/A), controlling glucose-evoked granule recruitment and regulating dopamine release, thus serving as a potential target molecule in the treatment of psychosis. In addition, recent researches have shown that SV2C regulates hypertension and accelerates venous thromboembolism (VTE) and coagulation pathways and may play roles in several non-nervous system diseases...
July 31, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28772011/brain-molecular-changes-and-behavioral-alterations-induced-by-propofol-anesthesia-exposure-in-peripubertal-rats
#14
Željko Pavković, Kosara Smiljanić, Selma Kanazir, Desanka Milanović, Vesna Pešić, Sabera Ruždijić
BACKGROUND: Propofol is commonly used in modern anesthesiology. Some findings suggest that it is highly addictive. AIM: In this study it was examined whether propofol anesthesia exposure was able to induce behavioral alterations and brain molecular changes already described in addictive drug usage in peripubertal rats, during the onset of mid/periadolescence as a developmental period with increasing vulnerability to drug addiction. METHODS: The expression of D1 dopamine receptor, a dopamine, and cAMP-regulated phosphoprotein with a Mr 32 000; Ca(2+) /calmodulin-dependent protein kinase IIα; and Finkel-Biskis-Jinkins murine osteosarcoma viral oncogene homolog-B was examined in peripubertal rats 4, 24, and 48 hour after propofol anesthesia exposure by Western blot and immunohistochemistry...
September 2017: Paediatric Anaesthesia
https://www.readbyqxmd.com/read/28766743/mouse-retinal-ganglion-cell-signalling-is-dynamically-modulated-through-parallel-anterograde-activation-of-cannabinoid-and-vanilloid-pathways
#15
Andrew O Jo, Jennifer M Noel, Monika Lakk, Oleg Yarishkin, Daniel A Ryskamp, Koji Shibasaki, Maureen A McCall, David Križaj
How retinal ganglion cells (RGCs) process and integrate synaptic, mechanical, swelling stimuli with light inputs is an area of intense debate. The nociceptive cation channel TRPV1 (transient receptor potential vanilloid type 1) modulates RGC Ca(2+) signals and excitability yet the proportion of RGCs that express it remains unclear. Further, TRPV1's response to endocannabinoids (eCBs), the putative endogenous retinal activators unknown, as is the potential modulation by cannabinoid receptors (CBRs). The expression of TRPV1 in RGCs from the Ai9:Trpv1 reporter mouse was nonuniform with peak density in the early- and mid-peripheral retina...
August 2, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28764937/distinctive-changes-of-l-type-calcium-channels-and-dopamine-receptors-in-the-dorsomedial-and-dorsolateral-striatum-after-the-expression-of-habitual-cocaine-seeking-behaviour-in-rats
#16
Fang Shen, Shubo Jin, Ying Duan, Jing Liang, Meng Zhang, Fengze Jiang, Nan Sui
Habitual drug-seeking behaviour is essential in the transition from recreational drug use to compulsive drug use and is regulated by the dopamine (DA) system of the dorsal striatum (DS). However, a comparative study of the two subtypes of DA receptors, D1 receptors (D1R) and D2 receptors (D2R), which have opposite regulatory functions, in habitual drug-seeking behaviour is absent. Moreover, the effects of L-type calcium channels (LTCCs) and the subtypes Cav1.2 and Cav1.3, which are downstream of D1R and D2R, respectively, on habitual drug-seeking behaviour have yet to be revealed...
July 29, 2017: Neuroscience
https://www.readbyqxmd.com/read/28758939/stonin-2-overexpression-is-correlated-with-unfavorable-prognosis-and-tumor-invasion-in-epithelial-ovarian-cancer
#17
Xiaoying Sun, Weijing Zhang, Han Li, Chunhao Niu, Yulan Ou, Libing Song, Yanna Zhang
Stonin 2 (STON2), which functions in adjusting endocytotic complexes, is probably involved in the monitoring of the internalization of dopamine D2 receptors which have an inhibitory action of dopamine on tumor progression. However, its clinical significance in tumor progression and prognosis remains unclear. We explored the association between STON2 and the clinicopathological characteristics of epithelial ovarian cancer (EOC). The STON2 levels in ovarian cancer and normal cell lines and tissues were detected by real-time PCR and Western blot analyses...
July 29, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28757212/bradykinin-b2-and-dopamine-d2-receptors-form-a-functional-dimer
#18
Anna Niewiarowska-Sendo, Agnieszka Polit, Monika Piwowar, Magdalena Tworzydło, Andrzej Kozik, Ibeth Guevara-Lora
In recent years a wide range of studies have shown that G protein-coupled receptors modulate a variety of cell functions through the formation of dimers. For instance, there is growing evidence for the dimerization of bradykinin or dopamine receptors, both as homodimers and heterodimers. A discovery of direct interactions of angiotensin II receptors with bradykinin 2 receptor (B2R) or dopamine D2 (D2R) receptor has led to a hypothesis on a potential dimerization between two latter receptors. In this study, we have demonstrated a constitutive colocalization of receptors on the membranes of HEK293 cells transiently transfected with plasmid vectors encoding B2R and D2R, fused with fluorescent proteins...
July 27, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28756461/adolescent-stress-leads-to-glutamatergic-disturbance-through-dopaminergic-abnormalities-in-the-prefrontal-cortex-of-genetically-vulnerable-mice
#19
Yurie Matsumoto, Minae Niwa, Akihiro Mouri, Yukihiro Noda, Takeshi Fukushima, Norio Ozaki, Toshitaka Nabeshima
BACKGROUND: Stress during the adolescent period influences postnatal maturation and behavioral patterns in adulthood. Adolescent stress-induced molecular and functional changes in neurons are the key clinical features of psychiatric disorders including schizophrenia. OBJECTIVE: In the present study, we exposed genetically vulnerable mice to isolation stress to examine the molecular changes in the glutamatergic system involving N-methyl-d-aspartate (NMDA) receptors via dopaminergic disturbance in the prefrontal cortex (PFc)...
July 29, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28755886/pharmacological-profile-of-mephedrone-analogs-and-related-new-psychoactive-substances
#20
REVIEW
Dino Luethi, Karolina E Kolaczynska, Luca Docci, Stephan Krähenbühl, Marius C Hoener, Matthias E Liechti
BACKGROUND: Mephedrone is a synthetic cathinone and one of the most popular recreationally used new psychoactive substances. The aim of the present study was to characterize the in vitro pharmacology of novel analogs of mephedrone and related newly emerged designer stimulants. METHODS: We determined norepinephrine, dopamine, and serotonin transporter inhibition potencies and monoamine release in transporter-transfected human embryonic kidney 293 cells. We also assessed monoamine receptor and transporter binding affinities...
July 26, 2017: Neuropharmacology
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