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dopamine 5 receptor

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https://www.readbyqxmd.com/read/29686613/essential-control-of-the-function-of-the-striatopallidal-neuron-by-pre-coupled-complexes-of-adenosine-a-2a-dopamine-d-2-receptor-heterotetramers-and-adenylyl-cyclase
#1
Sergi Ferré, Jordi Bonaventura, Wendy Zhu, Candice Hatcher-Solis, Jaume Taura, César Quiroz, Ning-Sheng Cai, Estefanía Moreno, Verónica Casadó-Anguera, Alexxai V Kravitz, Kimberly R Thompson, Dardo G Tomasi, Gemma Navarro, Arnau Cordomí, Leonardo Pardo, Carme Lluís, Carmen W Dessauer, Nora D Volkow, Vicent Casadó, Francisco Ciruela, Diomedes E Logothetis, Daniel Zwilling
The central adenosine system and adenosine receptors play a fundamental role in the modulation of dopaminergic neurotransmission. This is mostly achieved by the strategic co-localization of different adenosine and dopamine receptor subtypes in the two populations of striatal efferent neurons, striatonigral and striatopallidal, that give rise to the direct and indirect striatal efferent pathways, respectively. With optogenetic techniques it has been possible to dissect a differential role of the direct and indirect pathways in mediating "Go" responses upon exposure to reward-related stimuli and "NoGo" responses upon exposure to non-rewarded or aversive-related stimuli, respectively, which depends on their different connecting output structures and their differential expression of dopamine and adenosine receptor subtypes...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29683809/role-of-d1-like-and-d2-like-dopamine-receptors-within-the-ventral-tegmental-area-in-stress-induced-and-drug-priming-induced-reinstatement-of-morphine-seeking-in-rats
#2
Sharareh Farahimanesh, Marzieh Moradi, Farzaneh Nazari-Serenjeh, Shahram Zarrabian, Abbas Haghparast
The ventral tegmental area (VTA) as a major source of dopamine neurons projecting to cortical and limbic regions has a crucial role in reward as well as stress processes. Dopamine is a predominant neurotransmitter in the reward system, which plays an important role in both drug priming-induced and cue-induced reinstatement of cocaine and heroin seeking. It has been shown that this neurotransmitter has a role in stress-induced relapse to drug seeking. Therefore, the present study aims to evaluate the effects of intra-VTA administration of SCH-23390, as a dopamine D1-like receptor antagonist, and sulpiride, as a dopamine D2-like receptor antagonist, on drug priming-induced and food deprivation (FD)-induced reinstatement...
April 20, 2018: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29683325/a-thieno-2-3-d-pyrimidine-scaffold-is-a-novel-negative-allosteric-modulator-of-the-dopamine-d2-receptor
#3
Tim John Fyfe, Barbara Zarzycka, Herman D Lim, Barrie Kellam, Shailesh N Mistry, Vsevolod Katritch, Peter J Scammells, J Robert Lane, Ben Capuano
Recently, a novel negative allosteric modulator (NAM) of the D2 -like dopamine receptors 1 was identified through virtual ligand screening. This ligand comprises a thieno[2,3- d]pyrimidine scaffold that does not feature in known dopaminergic ligands. Herein, we provide pharmacological validation of an allosteric mode of action for 1, revealing that it is a NAM of dopamine efficacy and identify the structural determinants of this allostery. We find that key structural moieties are important for functional affinity and negative cooperativity, whilst functionalization of the thienopyrimidine at the 5- and 6-positions results in analogues with divergent cooperativity profiles...
April 23, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29681853/caffeine-promotes-conversion-of-palmitic-acid-to-palmitoleic-acid-by-inducing-expression-of-fat-5-in-caenorhabditis-elegans-and-scd1-in-mice
#4
Xiaocui Du, Qin Huang, Yun Guan, Ming Lv, Xiaofang He, Chongye Fang, Xuanjun Wang, Jun Sheng
The synthesis and metabolism of fatty acids in an organism is related to many biological processes and is involved in several diseases. The effects of caffeine on fatty acid synthesis and fat storage in Caenorhabditis elegans and mice were studied. After 6 h of food deprivation, adult C. elegans were treated with 0.1 mg/mL caffeine for 24 h. Quantitative reverse-transcription polymerase chain reaction showed that, among all the genes involved in fat accumulation, the mRNA expression of fat-5 in caffeine-treated C...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29680514/brain-blood-cerebrospinal-fluid-and-serum-biomarkers-in-schizophrenia
#5
REVIEW
Alireza Mohammadi, Ehsan Rashidi, Vahid Ghasem Amooeian
Over the last decade, finding a reliable biomarker for the early detection of schizophrenia (Scz) has been a topic of interest. The main goal of the current review is to provide a comprehensive view of the brain, blood, cerebrospinal fluid (CSF), and serum biomarkers of Scz disease. Imaging studies have demonstrated that the volumes of the corpus callosum, thalamus, hippocampal formation, subiculum, parahippocampal gyrus, superior temporal gyrus, prefrontal and orbitofrontal cortices, and amygdala-hippocampal complex were reduced in patients diagnosed with Scz...
April 13, 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29678723/modulatory-effect-of-dopamine-receptor-5-on-the-neurosecretory-dahlgren-cells-of-the-olive-flounder-paralichthys-olivaceus
#6
Zhaohui Lan, Wei Zhang, Jinling Xu, Mo Zhou, Yingxin Chen, Huafeng Zou, Weiqun Lu
A neuromodulatory role for dopamine has been reported for magnocellular neuroendocrine cells in the mammalian hypothalamus. We examined its potential role as a local intercellular messenger in the neuroendocrine Dahlgren cell population of the caudal neurosecretory system (CNSS) of the euryhaline flounder Paralichthys olivaceus. In vitro application of dopamine (DA) caused an increase in electrical activity (firing frequency, recorded extracellularly) of Dahlgren cells, recruitment of previously silent cells, together with a greater proportion of cells showing phasic (irregular) activity...
April 17, 2018: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/29677538/improvement-effects-of-a-mixed-extract-of-flowers-of-pueraria-thomsonii-benth-and-peels-of-citrus-unshiu-markovich-on-postmenopausal-symptoms-of-ovariectomized-mice
#7
Na-Ra Han, Sun-Young Nam, Sungwei Hong, Hee-Yun Kim, Phil-Dong Moon, Hyeong-Jin Kim, Hosong Cho, Boyoung Lee, Hyung-Min Kim, Hyun-Ja Jeong
BACKGROUND: Menopausal hot flushes occur frequently in postmenopausal women. In the present study, we investigated a regulatory effect of a mixed extract of flowers of Pueraria thomsonii Benth. and peels of Citrus unshiu Markovich (PCE17), an extract of flowers of Pueraria thomsonii Benth. (PE), an extract of peels of Citrus unshiu Markovich (CE), a mixture of tectorigenin 7-O-xylosylglucoside, tectoridin, and tectorigenin (Tec, the active compounds of PE), and hesperidin (Hes, an active compound of CE) on menopausal hot flushes...
April 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29671013/ontogeny-of-cocaine-induced-behaviors-and-cocaine-pharmacokinetics-in-male-and-female-neonatal-preweanling-and-adult-rats
#8
Sanders A McDougall, Matthew G Apodaca, Alena Mohd-Yusof, Adrian D Mendez, Caitlin G Katz, Angie Teran, Israel Garcia-Carachure, Anthony T Quiroz, Cynthia A Crawford
RATIONALE: Ontogenetic differences in the behavioral responsiveness to cocaine have often been attributed to the maturation of dopaminergic elements (e.g., dopamine transporters, D2High receptors, receptor coupling, etc.). OBJECTIVE: The purpose of this study was to determine whether ontogenetic changes in cocaine pharmacokinetics might contribute to age-dependent differences in behavioral responsiveness. METHODS: Male and female neonatal (PD 5), preweanling (PD 10 and PD 20), and adult (PD 70) rats were injected (IP) with cocaine or saline and various behaviors (e...
April 18, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29670116/association-between-radiological-parameters-and-clinical-and-molecular-characteristics-in-human-somatotropinomas
#9
María R Alhambra-Expósito, Alejandro Ibáñez-Costa, Paloma Moreno-Moreno, Esther Rivero-Cortés, Mari C Vázquez-Borrego, Cristóbal Blanco-Acevedo, Álvaro Toledano-Delgado, María S Lombardo-Galera, Juan A Vallejo-Casas, Manuel D Gahete, Justo P Castaño, María A Gálvez, Raúl M Luque
Acromegaly is a rare but severe disease, originated in 95% of cases by a growth hormone-secreting adenoma (somatotropinoma) in the pituitary. Magnetic resonance imaging (MRI) is a non-invasive technique used for the diagnosis and prognosis of pituitary tumours. The aim of this study was to determine whether the use of T2-weighted signal intensity at MRI could help to improve the characterisation of somatotropinomas, by analysing its relationship with clinical/molecular features. An observational study was implemented in a cohort of 22 patients (mean age = 42...
April 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29664745/cross-tolerance-between-nitric-oxide-synthase-inhibition-and-atypical-antipsychotics-modify-nicotinamide-adenine-dinucleotide-phosphate-diaphorase-activity-in-mouse-lateral-striatum
#10
Sonia G Prieto, João C S Silva, Mairon O de Lima, Maria C Almeida, Marcela B Echeverry
Previous research indicates that the subchronic administration of NG-nitro-L-arginine (L-NOARG) produces tolerance to haloperidol-induced catalepsy in Swiss mice. The present study aimed to further investigate whether intermittent subchronic systemic administration of L-NOARG induces tolerance to the cataleptic effects of haloperidol as well as olanzapine or clozapine (Clz) in C57Bl mice after subchronic administration for 5 consecutive days. Striatal FosB protein expression was measured in an attempt to gain further insights into striatal mechanisms in antipsychotic-induced extrapyramidal symptoms side effects...
April 16, 2018: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29660611/effect-of-in-vivo-exposure-to-ambient-fine-particles-pm-2-5-on-the-density-of-dopamine-d-2-like-receptors-and-dopamine-induced-35-s-gtp%C3%AE-s-binding-in-rat-prefrontal-cortex-and-striatum-membranes
#11
María-de-Los-Angeles Andrade-Oliva, Octavio-Gamaliel Aztatzi-Aguilar, Francisco García-Sierra, Andrea De Vizcaya-Ruiz, José-Antonio Arias-Montaño
Male Sprague-Dawley rats (8-9 weeks-old) were exposed for three days (acute exposure) or eight weeks (subchronic exposure) to purified air or concentrated ambient fine particles, PM2.5 (≤2.5 μm; 15 to 18-fold of ambient air; 370-445 μg/m3 ). In membranes from rat prefrontal cortex (PFC) or striatum, the density and function of dopamine D2 -like receptors (D2 Rs) were assessed by [3 H]-spiperone binding and dopamine-stimulated [35 S]-GTPγS binding, respectively. Glial activation was evaluated by immunoperoxidase labeling of the glial fibrillary acidic protein (GFAP)...
April 10, 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29658442/evaluation-of-in-silico-anti-parkinson-potential-of-%C3%AE-asarone
#12
Meenakshi Gupta, Kamal Kant, Ruchika Sharma, Anoop Kumar
INTRODUCTION: Parkinson's disease is affecting millions of people worldwide. The prevalence of Parkinson's disease is 0.3% globally, rising to 1% in more than 60 years of age and 4% in more than 80 years of age and the figures are thought to be doubled by 2030. Thus, there is a great need to identify novel therapeutic strategies or candidate drug molecule which can rescue neuronal degeneration. β-asarone has potential to act as a neuroprotective agent but regarding its role in Parkinson disease, very few reports are available...
April 16, 2018: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29618432/effects-of-single-administration-of-apomorphine-on-memory-and-monoamine-metabolism-a-dose-related-study
#13
Huma Ikram, Rumaisa Zakir, Darakhshan Jabeen Haleem
In the present study, we have monitored dose dependent effects of apomorphine on learning and memory. Behavioral sensitization and craving, which develop upon repeated treatment with dopamine receptor agonist apomorphine, are major limitations of the therapeutic use of apomorphine in Parkinson's patients. Effects of single (intraperitoneal) injection of apomorphine at different doses (i.e., 0.5, 1.0, & 2.0 mg/ml/kg) on locomotion in a familiar environment (Skinner's box) and memory in Morris water maze were investigated...
March 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29615922/sensory-processing-and-integration-at-the-carotid-body-tripartite-synapse-neurotransmitter-functions-and-effects-of-chronic-hypoxia
#14
REVIEW
Erin M Leonard, Shaima Salman, Colin A Nurse
Maintenance of homeostasis in the respiratory and cardiovascular systems depends on reflexes that are initiated at specialized peripheral chemoreceptors that sense changes in the chemical composition of arterial blood. In mammals, the bilaterally-paired carotid bodies (CBs) are the main peripheral chemoreceptor organs that are richly vascularized and are strategically located at the carotid bifurcation. The CBs contribute to the maintenance of O2 , CO2 /H+ , and glucose homeostasis and have attracted much clinical interest because hyperactivity in these organs is associated with several pathophysiological conditions including sleep apnea, obstructive lung disease, heart failure, hypertension, and diabetes...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29614490/in-utero-exposure-to-fine-particulate-matter-causes-hypertension-due-to-impaired-renal-dopamine-d1-receptor-in-offspring
#15
Zhengmeng Ye, Xi Lu, Yi Deng, Xinquan Wang, Shuo Zheng, Hongmei Ren, Miao Zhang, Tingting Chen, Pedro A Jose, Jian Yang, Chunyu Zeng
BACKGROUND/AIMS: Adverse environment in utero can modulate adult phenotypes including blood pressure. Fine particulate matter (PM2.5) exposure in utero causes hypertension in the offspring, but the exact mechanisms are not clear. Renal dopamine D1 receptor (D1R), regulated by G protein-coupled receptor kinase type 4 (GRK4), plays an important role in the regulation of renal sodium transport and blood pressure. In this present study, we determined if renal D1R dysfunction is involved in PM2...
March 21, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29593213/evidence-for-functional-pre-coupled-complexes-of-receptor-heteromers-and-adenylyl-cyclase
#16
Gemma Navarro, Arnau Cordomí, Verónica Casadó-Anguera, Estefanía Moreno, Ning-Sheng Cai, Antoni Cortés, Enric I Canela, Carmen W Dessauer, Vicent Casadó, Leonardo Pardo, Carme Lluís, Sergi Ferré
G protein-coupled receptors (GPCRs), G proteins and adenylyl cyclase (AC) comprise one of the most studied transmembrane cell signaling pathways. However, it is unknown whether the ligand-dependent interactions between these signaling molecules are based on random collisions or the rearrangement of pre-coupled elements in a macromolecular complex. Furthermore, it remains controversial whether a GPCR homodimer coupled to a single heterotrimeric G protein constitutes a common functional unit. Using a peptide-based approach, we here report evidence for the existence of functional pre-coupled complexes of heteromers of adenosine A2A receptor and dopamine D2 receptor homodimers coupled to their cognate Gs and Gi proteins and to subtype 5 AC...
March 28, 2018: Nature Communications
https://www.readbyqxmd.com/read/29589276/dipentylammonium-binds-to-the-sigma-1-receptor-and-protects-against-glutamate-toxicity-attenuates-dopamine-toxicity-and-potentiates-neurite-outgrowth-in-various-cultured-cell-lines
#17
James M Brimson, Stephen T Safrany, Heider Qassam, Tewin Tencomnao
Alzheimer's disease is a neurodegenerative disease that affects 44 million people worldwide, costing the world $605 billion to care for those affected not taking into account the physical and psychological costs for those who care for Alzheimer's patients. Dipentylammonium is a simple amine, which is structurally similar to a number of other identified sigma-1 receptor ligands with high affinities such as (2R-trans)-2butyl-5-heptylpyrrolidine, stearylamine and dodecylamine. This study investigates whether dipentylammonium is able to provide neuroprotective effects similar to those of sigma-1 receptor agonists such as PRE-084...
March 27, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29579709/the-novel-piperazine-containing-compound-lqfm018-necroptosis-cell-death-mechanisms-dopamine-d-4-receptor-binding-and-toxicological-assessment
#18
Fabiana Bettanin Costa, Alane P Cortez, Renato Ivan de Ávila, Flávio S de Carvalho, Wanessa M Andrade, Andrezza F da Cruz, Karinna B Reis, Ricardo Menegatti, Luciano M Lião, Luiz Antônio S Romeiro, François Noël, Carlos Alberto M Fraga, Eliezer J Barreiro, Germán Sanz, Marcella F Rodrigues, Boniek G Vaz, Marize Campos Valadares
Piperazine is a promising scaffold for drug development due to its broad spectrum of biological activities. Based on this, the new piperazine-containing compound LQFM018 (2) [ethyl 4-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate] was synthetized and some biological activities investigated. In this work, we described its ability to bind aminergic receptors, antiproliferative effects as well as the LQFM018 (2)-triggered cell death mechanisms, in K562 leukemic cells, by flow cytometric analyses...
March 23, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29577894/bilateral-quinolinic-acid-induced-lipid-peroxidation-decreased-striatal-monoamine-levels-and-neurobehavioral-deficits-are-ameliorated-by-gip-receptor-agonist-d-ala-2-gip-in-rat-model-of-huntington-s-disease
#19
Mahip K Verma, Rajan Goel, Krishnadas Nandakumar, Kumar V S Nemmani
Huntington's disease (HD) is an inherited complex progressive neurodegenerative disorder with an established etiopathology linked to neuronal oxidative stress and corticostriatal excitotoxicity. Present study explores the effects of glucose-dependent insulinotropic polypeptide (GIP) receptor agonist on the neurobehavioral sequelae of quinolinic acid-induced phenotype of Huntington's disease in rats. Bilateral administration of quinolinic acid (300 nmol/4µL) to the rat striatum led to characteristic deficits in, locomotor activity, motor coordination, neuromuscular coordination and short-term episodic memory...
March 22, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29572645/effects-of-the-serotonin-5-ht-1a-receptor-biased-agonists-f13714-and-f15599-on-striatal-neurotransmitter-levels-following-l-dopa-administration-in-hemi-parkinsonian-rats
#20
Adrian Newman-Tancredi, Mark A Varney, Andrew C McCreary
Peak-dose dyskinesia is associated with the dramatic increase in striatal dopamine levels that follows L-DOPA administration. The 'false neurotransmitter' hypothesis postulates that the latter is likely due to an aberrant processing of L-DOPA by serotonergic neurons. In keeping with this hypothesis, two highly selective 'biased agonists' of 5-HT1A receptors-namely F13714 and F15599 (NLX-101)-were recently shown to exhibit exceptionally potent anti-dyskinetic activity without impairing L-DOPA therapeutic properties despite their differential targeting of 5-HT1A receptor sub-populations...
March 23, 2018: Neurochemical Research
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