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Dopamine antagonists

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https://www.readbyqxmd.com/read/28340290/nucleus-accumbens-dopamine-receptors-mediate-hypothalamus-induced-antinociception-in-the-rat-formalin-test
#1
A Siahposht-Khachaki, P Pourreza, S Ezzatpanah, A Haghparast
BACKGROUND: Lateral hypothalamus (LH) involves in modulation of tonic pain. Regarding the direct and indirect neural connections between the LH and nucleus accumbens (NAc), we aimed to examine the pain modulatory role of NAc dopamine receptors in modulation of LH-induced analgesia in the formalin test. METHODS: Vehicle-control groups received saline or DMSO into the NAc and saline into the LH. Carbachol-control groups received carbachol (250 nmol/L) into the LH, 5 min after saline or DMSO injection into the NAc...
March 24, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28327597/molecular-signaling-underlying-bulleyaconitine-a-baa-induced-microglial-expression-of-prodynorphin
#2
Teng-Fei Li, Hai-Yun Wu, Yi-Rui Wang, Xin-Yan Li, Yong-Xiang Wang
Bulleyaconitine (BAA) has been shown to possess antinociceptive activities by stimulation of dynorphin A release from spinal microglia. This study investigated its underlying signal transduction mechanisms. The data showed that (1) BAA treatment induced phosphorylation of CREB (rather than NF-κB) and prodynorphin expression in cultured primary microglia, and antiallodynia in neuropathy, which were totally inhibited by the CREB inhibitor KG-501; (2) BAA upregulated phosphorylation of p38 (but not ERK or JNK), and the p38 inhibitor SB203580 (but not ERK or JNK inhibitor) and p38β gene silencer siRNA/p38β (but not siRNA/p38α) completely blocked BAA-induced p38 phosphorylation and/or prodynorphin expression, and antiallodynia; (3) BAA stimulated cAMP production and PKA phosphorylation, and the adenylate cyclase inhibitor DDA and PKA inhibitor H-89 entirely antagonized BAA-induced prodynorphin expression and antiallodynia; (4) The Gs-protein inhibitor NF449 completely inhibited BAA-increased cAMP level, prodynorphin expression and antiallodynia, whereas the antagonists of noradrenergic, corticotrophin-releasing factor, A1 adenosine, formyl peptide, D1/D2 dopamine, and glucagon like-peptide-1 receptors failed to block BAA-induced antiallodynia...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28327307/discovery-characterization-and-biological-evaluation-of-a-novel-r-4-4-difluoropiperidine-scaffold-as-dopamine-receptor-4-d4r-antagonists
#3
Daniel E Jeffries, Jonathan O Witt, Andrea L McCollum, Kayla J Temple, Miguel A Hurtado, Joel M Harp, Anna L Blobaum, Craig W Lindsley, Corey R Hopkins
Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4 receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.
December 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28326743/dopamine-receptors-modulate-t-lymphocytes-via-inhibition-of-camp-creb-signaling-pathway
#4
(no author information available yet)
OBJECTIVES: We have previously reported that dopamine D2-like receptors including D2, D3 and D4 receptors are more important in mediating modulation of T cells than dopamine D1-like receptors (D1 and D5 receptors). Here we aimed to clarify the role of D2-like receptors in regulation of differentiation and function of T lymphocyte subsets, including helper T (Th)1, Th2, Th17 and regulatory T (Treg) cells. METHODS: Lymphocytes, separated from the mesenteric lymph nodes of mice, were stimulated with concanavalin A (Con A) and treated with the D2-like receptor agonist quinpirole or the antagonist haloperidol...
December 22, 2016: Neuro Endocrinology Letters
https://www.readbyqxmd.com/read/28323029/the-dopamine-d3-receptor-antagonists-pg01037-ngb2904-sb277011a-and-u99194-reverse-abcg2-transporter-mediated-drug-resistance-in-cancer-cell-lines
#5
Noor Hussein, Haneen Amawi, Chandrabose Karthikeyan, F Scott Hall, Roopali Mittal, Piyush Trivedi, Charles R Ashby, Amit K Tiwari
THE ATP: binding cassette (ABC) family G2 (ABCG2) transporters are known to produce multidrug resistance (MDR) in cancer, thereby limiting the clinical response to chemotherapy. Molecular modeling data indicated that certain dopamine (DA) D3 receptor antagonists had a significant binding affinity for ABCG2 transporter. Therefore, in this in vitro study, we determined the effect of the D3 receptor antagonists PG01037, NGB2904, SB277011A, and U99194 on MDR resulting from the overexpression of ABCG2 transporters...
March 16, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28322273/neuregulin-2-ablation-results-in-dopamine-dysregulation-and-severe-behavioral-phenotypes-relevant-to-psychiatric-disorders
#6
L Yan, A Shamir, M Skirzewski, E Leiva-Salcedo, O B Kwon, I Karavanova, D Paredes, O Malkesman, K R Bailey, D Vullhorst, J N Crawley, A Buonanno
Numerous genetic and functional studies implicate variants of Neuregulin-1 (NRG1) and its neuronal receptor ErbB4 in schizophrenia and many of its endophenotypes. Although the neurophysiological and behavioral phenotypes of NRG1 mutant mice have been investigated extensively, practically nothing is known about the function of NRG2, the closest NRG1 homolog. We found that NRG2 expression in the adult rodent brain does not overlap with NRG1 and is more extensive than originally reported, including expression in the striatum and medial prefrontal cortex (mPFC), and therefore generated NRG2 knockout mice (KO) to study its function...
March 21, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28319198/methamphetamine-induces-shati-nat8l-expression-in-the-mouse-nucleus-accumbens-via-creb-and-dopamine-d1-receptor-dependent-mechanism
#7
Kyosuke Uno, Toh Miyazaki, Kengo Sodeyama, Yoshiaki Miyamoto, Atsumi Nitta
Shati/Nat8L significantly increased in the nucleus accumbens (NAc) of mice after repeated methamphetamine (METH) treatment. We reported that Shati/Nat8L overexpression in mouse NAc attenuated METH-induced hyperlocomotion, locomotor sensitization, and conditioned place preference. We recently found that Shati/Nat8L overexpression in NAc regulates the dopaminergic neuronal system via the activation of group II mGluRs by elevated N-acetylaspartylglutamate following N-acetylaspartate increase due to the overexpression...
2017: PloS One
https://www.readbyqxmd.com/read/28316587/characterization-of-the-antinociceptive-mechanisms-of-khat-extract-catha-edulis-in-mice
#8
Elham A Afify, Huda M Alkreathy, Ahmed S Ali, Hassan A Alfaifi, Lateef M Khan
This study investigated the antinociceptive mechanisms of khat extract (100, 200, and 400 mg/kg, i.p.) in four pain models: two thermic (hot plate, tail-flick) and two chemical (acetic acid, formalin) models. Male mice were pretreated intraperitoneally (i.p.) with the opioid receptor blocker naloxone (5 mg/kg), the cholinergic antagonist atropine (2 mg/kg), the selective α1 blocker prazosin (1 mg/kg), the dopamine D2 antagonist haloperidol (1.5 mg/kg), or the GABAA receptor antagonist, bicuculline (1 mg/kg) 15 minutes prior to i...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28304244/intravitreally-administered-dopamine-d2-like-and-d4-but-not-d1-like-receptor-agonists-reduce-form-deprivation-myopia-in-tree-shrews
#9
Alexander H Ward, John T Siegwart, Michael R Frost, Thomas T Norton
We examined the effect of intravitreal injections of D1-like and D2-like dopamine receptor agonists and antagonists and D4 receptor drugs on form-deprivation myopia (FDM) in tree shrews, mammals closely related to primates. In eleven groups (n = 7 per group), we measured the amount of FDM produced by monocular form deprivation (FD) over an 11-day treatment period. The untreated fellow eye served as a control. Animals also received daily 5 µL intravitreal injections in the FD eye. The reference group received 0...
January 2017: Visual Neuroscience
https://www.readbyqxmd.com/read/28302436/pharmacological-characterization-of-dopamine-receptors-in-the-rice-striped-stem-borer-chilo-suppressalis
#10
Gang Xu, Shun-Fan Wu, Gui-Xiang Gu, Zi-Wen Teng, Gong-Yin Ye, Jia Huang
Dopamine is an important neurotransmitter and neuromodulator in both vertebrates and invertebrates and is the most abundant monoamine present in the central nervous system of insects. A complement of functionally distinct dopamine receptors mediate the signal transduction of dopamine by modifying intracellular Ca(2+) and cAMP levels. In the present study, we pharmacologically characterized three types of dopamine receptors, CsDOP1, CsDOP2 and CsDOP3, from the rice striped stem borer, Chilo suppressalis. All three receptors show considerable sequence identity with orthologous dopamine receptors...
March 14, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28300546/cocaine-self-administration-specifically-increases-a2ar-d2r-and-d2r-sigma1r-heteroreceptor-complexes-in-the-rat-nucleus-accumbens-shell-relevance-for-cocaine-use-disorder
#11
Dasiel O Borroto-Escuela, Manuel Narváez, Karolina Wydra, Julia Pintsuk, Luca Pinton, Antonio Jimenez-Beristain, Michael Di Palma, Joanna Jastrzębska, Malgorzata Filip, Kjell Fuxe
Adenosine 2A receptor (A2AR) agonists were indicated to reduce cocaine reward and cocaine seeking mainly through activation of antagonistic allosteric A2AR-dopamine D2R (D2R) interactions in A2AR-D2R heteroreceptor complexes. Furthermore, it was shown that modulation of cocaine reward involves antagonistic A2AR-D2R interactions in the ventral but not the dorsal striatum in rats. In the current work the proximity ligation assay (PLA) was used to further study the A2AR-D2R heteroreceptor complexes in the nucleus accumbens shell and core as well as the dorsal striatum under the influence of cocaine self-administration in rats...
March 12, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28298165/high-throughput-patch-clamp-screening-in-human-%C3%AE-6-containing-nicotinic-acetylcholine-receptors
#12
Lucas C Armstrong, Glenn E Kirsch, Nikolai B Fedorov, Caiyun Wu, Yuri A Kuryshev, Abby L Sewell, Zhiqi Liu, Arianne L Motter, Carmine S Leggett, Michael S Orr
Nicotine, the addictive component of tobacco products, is an agonist at nicotinic acetylcholine receptors (nAChRs) in the brain. The subtypes of nAChR are defined by their α- and β-subunit composition. The α6β2β3 nAChR subtype is expressed in terminals of dopaminergic neurons that project to the nucleus accumbens and striatum and modulate dopamine release in brain regions involved in nicotine addiction. Although subtype-dependent selectivity of nicotine is well documented, subtype-selective profiles of other tobacco product constituents are largely unknown and could be essential for understanding the addiction-related neurological effects of tobacco products...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28291301/-acute-dystonia-due-to-aripiprazole-use-in-two-children-with-autism-spectrum-disorder-in-the-first-five-years-of-life
#13
Mustafa Küçükköse, Bürge Kabukçu Başay
Autism spectrum disorders (ASD) are neuropsychiatric disorders characterized by impairment in social interactions, in verbal and non-verbal communication, and restricted and stereotyped patterns of interest and behavior within the first 3 years of life. Pharmacologic interventions may be needed for the treatment of temper tantrums, aggression, hyperactivity, and stereotypes in children with ASD. The approval of aripiprazole by the United States Food and Drug Administration (USFDA) for the treatment of temper tantrums in children and adolescents with ASD has gained increased interest for the use in these patients...
2017: Türk Psikiyatri Dergisi, Turkish Journal of Psychiatry
https://www.readbyqxmd.com/read/28289795/-pharmacological-treatment-of-motor-symptoms-in-parkinson-s-diseases
#14
W H Jost
Since the 1960s many substance classes have been introduced for treatment of idiopathic Parkinson's disease. The most important and effective medication is levodopa (L-dopa) always in combination with a decarboxylase inhibitor. In addition, dopamine agonists, monoamine oxidase B (MAO-B) inhibitors, catechol-o-methyltransferase (COMT) inhibitors, N‑methyl-D-aspartate (NMDA) antagonists and very rarely anticholinergics are administered depending on the motor symptoms, age and a multitude of other factors. Fortunately, within the substance classes there are various preparations, which also have different effects...
March 13, 2017: Der Nervenarzt
https://www.readbyqxmd.com/read/28289242/acupuncture-attenuated-vascular-dementia-induced-hippocampal-long-term-potentiation-impairments-via-activation-of-d1-d5-receptors
#15
Yang Ye, Hui Li, Jing-Wen Yang, Xue-Rui Wang, Guang-Xia Shi, Chao-Qun Yan, Si-Ming Ma, Wen Zhu, Qian-Qian Li, Tian-Ran Li, Ling-Yong Xiao, Cun-Zhi Liu
BACKGROUND AND PURPOSE: Emerging evidence suggests that acupuncture could improve cognitive impairment in vascular dementia by enhancing synaptic plasticity in the hippocampus. The purpose of this study is to investigate whether dopamine, a key mediator of synaptic plasticity, is involved in this cognitive improvement. METHODS: Vascular dementia model was established by bilateral common carotid arteries occlusion in male Wistar rats. Three days after the operation, animals received acupuncture treatment for 2 weeks, once daily...
March 13, 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/28288863/toluene-s-effects-on-activity-and-extracellular-dopamine-in-the-mouse-are-altered-by-gabaa-antagonism
#16
Sean P Callan, Aaron K Apawu, Tiffany A Mathews, Scott E Bowen
The abuse of inhalants like toluene continues to be widespread around the world, especially among children and teenagers. Despite its frequency of misuse, the dynamics between dopamine (DA) and gamma-aminobutyric acid (GABA) in response to toluene exposure remains unclear. To further decipher toluene's actions, we used a dynamic exposure system in combination with microdialysis to examine in vivo the effects of acutely inhaled toluene on DA release within the mouse caudate putamen (CPu). Results show that toluene inhalation produced increases in DA levels and locomotor activity...
March 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28285123/preclinical-predictors-that-the-orthosteric-mglu2-3-receptor-antagonist-ly3020371-will-not-engender-ketamine-associated-neurotoxic-motor-cognitive-subjective-or-abuse-liability-related-effects
#17
J M Witkin, J A Monn, J Li, B Johnson, D L McKinzie, X-S Wang, B A Heinz, R Li, P L Ornstein, S C Smith, C H Mitch, D O Calligaro, S Swanson, D Allen, K Phillips, G Gilmour
The novel mGlu2/3 receptor antagonist, LY3020371 has been shown to produce antidepressant-like effects comparable to that of the clinically-effective antidepressant ketamine. In the present study, we investigated whether LY3020371 would be predicted to be free of the side-effects and safety pharmacology issues associated with ketamine. In contrast to ketamine, LY3020371 produced small increases in locomotion and did not impair motor performance on an inverted. Ketamine, but not LY3020371, increased dopamine efflux in the nucleus accumbens of rats...
March 8, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28284952/importance-of-d1-and-d2-receptor-stimulation-for-the-induction-and-expression-of-cocaine-induced-behavioral-sensitization-in-preweanling-rats
#18
Sanders A McDougall, Krista N Rudberg, Ana Veliz, Janhavi M Dhargalkar, Aleesha S Garcia, Loveth C Romero, Ashley E Gonzalez, Alena Mohd-Yusof, Cynthia A Crawford
The behavioral manifestations of psychostimulant-induced sensitization vary markedly between young and adult rats, suggesting that the neural mechanisms mediating this phenomenon differ across ontogeny. In this project we examined the importance of D1 and D2 receptors for the induction and expression of cocaine-induced behavioral sensitization during the preweanling period. In the behavioral experiments, rats were injected with reversible D1 and/or D2 antagonists (SCH23390 and/or raclopride) or an irreversible receptor antagonist (EEDQ) either before cocaine administration on the pretreatment day (induction) or before cocaine challenge on the test day (expression)...
March 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28283756/dopamine-t-cells-and-multiple-sclerosis-ms
#19
REVIEW
Mia Levite, Franca Marino, Marco Cosentino
Dopamine is a key neurotransmitter that induces critical effects in the nervous system and in many peripheral organs, via 5 dopamine receptors (DRs): D1R-D5R. Dopamine also induces many direct and very potent effects on many DR-expressing immune cells, primarily T cells and dendritic cells. In this review, we focus only on dopamine receptors, effects and production in T cells. Dopamine by itself (at an optimal concentration of~0.1 nM) induces multiple function of resting normal human T cells, among them: T cell adhesion, chemotactic migration, homing, cytokine secretion and others...
March 10, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28280480/the-efficacy-and-tolerability-of-the-clonidine-transdermal-patch-in-the-treatment-for-children-with-tic-disorders-a-prospective-open-single-group-self-controlled-study
#20
Pan-Pan Song, Li Jiang, Xiu-Juan Li, Si-Qi Hong, Shuang-Zi Li, Yue Hu
BACKGROUND: To evaluate the efficacy and tolerability of a clonidine transdermal patch in the treatment of children with tic disorders (TD) and to establish a predictive model for patients. METHODS: Forty-one patients who met the inclusion criteria entered into 12 weeks of prospective, open, single-group, self-controlled treatment with a clonidine transdermal patch. The Yale Global Tic Severity Scale (YGTSS) was employed before therapy (baseline) and at 4, 8, and 12 weeks after therapy...
2017: Frontiers in Neurology
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