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Dopamine receptor 2

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https://www.readbyqxmd.com/read/29352161/the-action-of-a-negative-allosteric-modulator-at-the-dopamine-d2-receptor-is-dependent-upon-sodium-ions
#1
Christopher J Draper-Joyce, Ravi Kumar Verma, Mayako Michino, Jeremy Shonberg, Anitha Kopinathan, Carmen Klein Herenbrink, Peter J Scammells, Ben Capuano, Ara M Abramyan, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R). Experimental and computational evidences have revealed that this effect is mediated by the binding of Na+ to a conserved site located beneath the orthosteric binding site (OBS). SB269652 acts as a negative allosteric modulator (NAM) of the D2R that adopts an extended bitopic pose, in which the tetrahydroisoquinoline moiety interacts with the OBS and the indole-2-carboxamide moiety occupies a secondary binding pocket (SBP)...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29346639/comparison-of-dopamine-d3-and-d2-receptor-occupancies-by-a-single-dose-of-blonanserin-in-healthy-subjects-a-positron-emission-tomography-study-with-11c-phno
#2
Amane Tateno, Takeshi Sakayori, Woo-Chan Kim, Kazuyoshi Honjo, Haruo Nakayama, Ryosuke Arakawa, Yoshiro Okubo
Background: Blockade of D3 receptor, a member of the dopamine D2-like receptor family, has been suggested as a possible medication for schizophrenia. Blonanserin has high affinity in vitro for D3 as well as D2 receptors. We investigated whether a single dose of 12 mg blonanserin, which was within the daily clinical dose range (i.e., 8-24 mg) for the treatment of schizophrenia, occupies D3 as well as D2 receptors in healthy subjects. Methods: Six healthy males (mean 35...
January 13, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29346545/influence-of-nicotine-metabolism-ratio-on-11c-phno-pet-binding-in-tobacco-smokers
#3
Patricia Di Ciano, Rachel F Tyndale, Esmaeil Mansouri, Christian S Hendershot, Alan A Wilson, Dina Lagzdins, Sylvain Houle, Isabelle Boileau, Bernard Le Foll
Background: Identifying the biological basis of smoking cessation success is of growing interest. The rate of nicotine metabolism, measured by the nicotine metabolite ratio (NMR), affects multiple aspects of nicotine dependence. Fast nicotine metabolizers (FM) tend to smoke more, experience more withdrawal and craving and have lower cessation rates as compared to slow metabolizers (SM). The NMR predicts treatment response, and differences in brain activation between FM and SM have been reported in fMRI studies...
January 13, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29344260/dr2-blocker-thioridazine-a-promising-drug-for-ovarian-cancer-therapy
#4
Min Yong, Tinghe Yu, Si Tian, Shuaibin Liu, Jiao Xu, Jianguo Hu, Lina Hu
Dopamine receptor 2 (DR2) may be a biomarker for various types of cancer. Ovarian cancer cells overexpress DR2; therefore, blocking DR2 may be a novel treatment strategy for ovarian cancer. Thioridazine, a DR2 blocker, has antineoplastic activity in a variety of cancer cells. In view of the requirement for novel therapeutic agents in ovarian cancer, the present study aimed to determine the potential effects of thioridazine in vitro and in vivo. It was revealed that the DR2 blocker thioridazine induced cell death in a dose-dependent manner in ovarian cancer cells...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29342497/non-antipsychotic-catecholaminergic-drugs-for-antipsychotic-induced-tardive-dyskinesia
#5
REVIEW
Hany G El-Sayeh, John Rathbone, Karla Soares-Weiser, Hanna Bergman
BACKGROUND: Tardive dyskinesia (TD) is a disabling movement disorder associated with the prolonged use of antipsychotic medication. Several strategies have been examined in the treatment of TD. Currently, however, there is no clear evidence of the effectiveness of these drugs in TD and they have been associated with many side effects. One particular strategy would be to use pharmaceutical agents which are known to influence the catecholaminergic system at various junctures. OBJECTIVES: 1...
January 18, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29337986/the-e2-65a-mutation-disrupts-dynamic-binding-poses-of-sb269652-at-the-dopamine-d2-and-d3-receptors
#6
Ravi Kumar Verma, Ara M Abramyan, Mayako Michino, R Benjamin Free, David R Sibley, Jonathan A Javitch, J Robert Lane, Lei Shi
The dopamine D2 and D3 receptors (D2R and D3R) are important targets for antipsychotics and for the treatment of drug abuse. SB269652, a bitopic ligand that simultaneously binds both the orthosteric binding site (OBS) and a secondary binding pocket (SBP) in both D2R and D3R, was found to be a negative allosteric modulator. Previous studies identified Glu2.65 in the SBP to be a key determinant of both the affinity of SB269652 and the magnitude of its cooperativity with orthosteric ligands, as the E2.65A mutation decreased both of these parameters...
January 16, 2018: PLoS Computational Biology
https://www.readbyqxmd.com/read/29337226/glp-1-signaling-and-alcohol-mediated-behaviors-preclinical-and-clinical-evidence
#7
REVIEW
Elisabet Jerlhag
Alcohol addiction, affecting approximately four percent of the population, contributes significantly to the global burden of diseases and is a substantial cost to the society. The neurochemical mechanisms regulating alcohol mediated behaviors is complex and in more recent years a new physiological role of the gut-brain peptides, traditionally known to regulate appetite and food intake, have been suggested. Indeed, regulators of alcohol-mediated behaviors. One of these gut-brain peptides is the annorexigenic peptide glucagon-like peptide-1 (GLP-1), Preclinical studies show that GLP-1 receptor activation, either by GLP-1 or analogues, attenuate the ability of alcohol to activate the mesolimbic dopamine system as well as decrease alcohol consumption and operant self-administration...
January 11, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29332198/drug-delivery-and-transport-into-the-central-circulation-an-example-of-zero-order-in-vivo-absorption-of-rotigotine-from-a-transdermal-patch-formulation
#8
Willi Cawello, Marina Braun, Jens-Otto Andreas
BACKGROUND AND OBJECTIVE: Pharmacokinetic studies using deconvolution methods and non-compartmental analysis to model clinical absorption of drugs are not well represented in the literature. The purpose of this research was (1) to define the system of equations for description of rotigotine (a dopamine receptor agonist delivered via a transdermal patch) absorption based on a pharmacokinetic model and (2) to describe the kinetics of rotigotine disposition after single and multiple dosing...
January 13, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29324468/switching-antipsychotic-treatment-to-aripiprazole-in-psychotic-patients-with-neuroleptic-induced-tardive-dyskinesia-a-24-week-follow-up-study
#9
Chia-Hsiang Chan, Hung-Yu Chan, Yen-Ching Chen
Aripiprazole is a second-generation antipsychotics, acting as a partial dopamine D2 receptor agonist. Previous studies on aripiprazole for tardive dyskinesia (TD) treatment were limited and inconclusive. This study was aimed to examine the effectiveness of aripiprazole in psychotic patients with a pre-existing TD. This was an open-label 24-week prospective cohort study conducted in a public mental hospital in Northern Taiwan from January 2009 to February 2010.Psychotic patients were cross-titrated of prior antipsychotics with aripiprazole, and the severity of TD was assessed at baseline and at weeks 2, 4, 8, 12, 16, 20, and 24...
January 10, 2018: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29324345/synthesis-and-biological-evaluation-of-a-series-of-multi-target-n-substituted-cyclic-imide-derivatives-with-potential-antipsychotic-effect
#10
Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, Jianfeng Li, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang
In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D2/5-HT1A/5-HT2A receptors, but also endowed with low to moderate activities on 5-HT2C, H1, α1A, M3 receptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation...
January 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29320746/sada-expressing-staphylococci-in-the-human-gut-show-increased-cell-adherence-and-internalization
#11
Arif Luqman, Mulugeta Nega, Minh-Thu Nguyen, Patrick Ebner, Friedrich Götz
A subgroup of biogenic amines, the so-called trace amines (TAs), are produced by mammals and bacteria and can act as neuromodulators. In the genus Staphylococcus, certain species are capable of producing TAs through the activity of staphylococcal aromatic amino acid decarboxylase (SadA). SadA decarboxylates aromatic amino acids to produce TAs, as well as dihydroxy phenylalanine and 5-hydroxytryptophan to thus produce the neurotransmitters dopamine and serotonin. SadA-expressing staphylococci were prevalent in the gut of most probands, where they are part of the human intestinal microflora...
January 9, 2018: Cell Reports
https://www.readbyqxmd.com/read/29317484/chemogenetic-excitation-of-accumbens-projecting-infralimbic-cortical-neurons-blocks-toluene-induced-conditioned-place-preference
#12
Wesley N Wayman, John J Woodward
Abuse rates for inhalants among adolescents continue to be high, yet preclinical models for studying mechanisms underlying inhalant abuse remain limited. Our lab has previously shown that, in male rats, an acute binge-like exposure to toluene vapor that mimics human solvent abuse modifies the intrinsic excitability of medial prefrontal cortex (mPFC) pyramidal neurons projecting to the nucleus accumbens (NAc). These changes showed region (infralimbic; IL vs. prelimbic; PRL), layer (shallow; 2/3 vs. deep; 5/6), target (core vs...
January 9, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29305920/nicotinic-acetylcholine-receptor-nachr-mediated-dopamine-release-in-larval-drosophila-melanogaster
#13
Poojan Pyakurel, Mimi Shin, B Jill Venton
Acetylcholine is an excitatory neurotransmitter in the central nervous system of insects and the nicotinic acetylcholine receptor (nAChR) is a target for neonicotinoid insecticides. Functional insect nAChRs are difficult to express in host cells, and hence difficult to study. In mammals, acetylcholine and nicotine evoke dopamine release, but the extent to which this mechanism is conserved in insects is unknown. In intact larval ventral nerve cords (VNCs), we studied dopamine evoked by acetylcholine, nicotine, or neonicotinoids...
January 3, 2018: Neurochemistry International
https://www.readbyqxmd.com/read/29304113/discovery-of-indolylpiperazinylpyrimidines-with-dual-target-profiles-at-adenosine-a2a-and-dopamine-d2-receptors-for-parkinson-s-disease-treatment
#14
Yi-Ming Shao, Xiaohua Ma, Priyankar Paira, Aaron Tan, Deron Raymond Herr, Kah Leong Lim, Chee Hoe Ng, Gopalakrishnan Venkatesan, Karl-Norbert Klotz, Stephanie Federico, Giampiero Spalluto, Siew Lee Cheong, Yu Zong Chen, Giorgia Pastorin
Parkinson's disease (PD) is a neurodegenerative disorder characterized by progressive loss of dopaminergic neurons in the substantia nigra of the human brain, leading to depletion of dopamine production. Dopamine replacement therapy remains the mainstay for attenuation of PD symptoms. Nonetheless, the potential benefit of current pharmacotherapies is mostly limited by adverse side effects, such as drug-induced dyskinesia, motor fluctuations and psychosis. Non-dopaminergic receptors, such as human A2A adenosine receptors, have emerged as important therapeutic targets in potentiating therapeutic effects and reducing the unwanted side effects...
2018: PloS One
https://www.readbyqxmd.com/read/29299155/neuroprotection-by-aripiprazole-against-%C3%AE-amyloid-induced-toxicity-by-p-ck2%C3%AE-activation-via-inhibition-of-gsk-3%C3%AE
#15
So Youn Park, Hwa Kyoung Shin, Won Suk Lee, Sun Sik Bae, Koanhoi Kim, Ki Whan Hong, Chi Dae Kim
Psychosis is reported over 30% of patients with Alzheimer's disease (AD) in clinics. Aripiprazole is an atypical antipsychotic drug with partial agonist activity at the D2 dopamine and 5-HT1A receptors with low side-effect profile. We identified aripiprazole is able to overcome the amyloid-β (Aβ)-evoked neurotoxicity and then increase the cell viability. This study elucidated the mechanism(s) by which aripiprazole ameliorates Aβ1-42-induced decreased neurite outgrowth and viability in neuronal cells. Pretreatment with aripiprazole increased Brain-derived neurotrophic factor (BDNF) mRNA and protein expressions in N2a cells...
December 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/29288746/a-new-synthetic-drug-5-2-aminopropyl-indole-5-it-induces-rewarding-effects-and-increases-dopamine-d1-receptor-and-dopamine-transporter-mrna-levels
#16
Chrislean Jun Botanas, Seong Shoon Yoon, June Bryan de la Peña, Irene Joy Dela Peña, Mikyung Kim, Raly James Custodio, Taeseon Woo, Joung-Wook Seo, Choon-Gon Jang, Ji Seul Yang, Yoon Mi Yoon, Yong Sup Lee, Hee Jin Kim, Jae Hoon Cheong
In recent years, there has been a marked increase in the use of recreational synthetic psychoactive substances, which is a cause of concern among healthcare providers and legal authorities. In particular, there have been reports on the misuse of 5-(2-aminopropyl)indole (5-API; 5-IT), a new synthetic drug, and of fatal and non-fatal intoxication. Despite these reports, little is known about its psychopharmacological effects and abuse potential. Here, we investigated the abuse potential of 5-IT by evaluating its rewarding and reinforcing effects through conditioned place preference (CPP) (1, 10, and 30 mg/kg, i...
December 27, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29282344/-symptoms-and-pathophysiology-of-dyskinesias
#17
Masahiko Tomiyama
Symptomatic characteristics and recent advances in understanding the pathophysiology of tardive dyskinesias and levodopa-induced dyskinesias were reviewed. After the advent of atypical antipsychotics, tardive dyskinesias became less frequent, at least as observed during a short-term follow up. The dopamine supersensitivity hypothesis stating that blockade of dopamine D2 receptors by antipsychotics makes D2 receptors more sensitive to dopamine, has long been proposed. However, the true mechanisms remain to be determined...
December 2017: Brain and Nerve, Shinkei Kenkyū No Shinpo
https://www.readbyqxmd.com/read/29278360/a-concise-review-of-the-conflicting-roles-of-dopamine-1-versus-dopamine-2-receptors-in-wound-healing
#18
REVIEW
Alexandra R Vaughn, Michael James Davis, Raja K Sivamani, Roslyn Rivkah Isseroff
Catecholamines play an important regulatory role in cutaneous wound healing. The exact role of dopamine in human epidermis has yet to be fully elucidated. Current published evidence describes its differential effects on two separate families of G protein coupled receptors: D1-like and D2-like dopamine receptors. Dopamine may enhance angiogenesis and wound healing through its action on dopamine D1 receptors, while impairing wound healing when activating D2 receptors. This review summarizes the evidence for the role of dopamine in wound healing and describes potential mechanisms behind its action on D1 versus D2-like receptors in the skin...
December 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29278206/a-systematic-review-of-evidence-based-treatment-strategies-for-obsessive-compulsive-disorder-resistant-to-first-line-pharmacotherapy
#19
Umberto Albert, Donatella Marazziti, Gabriele Di Salvo, Francesca Solia, Gianluca Rosso, Giuseppe Maina
BACKGROUND: Serotonin reuptake inhibitors (SRIs) and cognitive-behavioral psychotherapy (CBT) are first-line treatments for obsessive-compulsive disorder (OCD). However, a significant proportion of patients do not respond satisfactorily to first-choice treatments. Several options have been investigated for the management of resistant patients. OBJECTIVE: The aim of the present paper is to systematically review the available literature concerning the strategies for the treatment of resistant adult patients with OCD...
December 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29274752/chronic-paroxetine-treatment-prevents-disruption-of-methamphetamine-sensitive-circadian-oscillator-in-a-transgenic-mouse-model-of-huntington-s-disease
#20
Koliane Ouk, Juliet Aungier, Marc Cuesta, A Jennifer Morton
Circadian abnormalities seen in Huntington's disease (HD) patients are recapitulated in several HD transgenic mouse models. In mice, alongside the master clock located in the suprachiasmatic nucleus (SCN), two other oscillators may influence circadian behaviour. These are the food-entrainable oscillator (FEO) and the methamphetamine-sensitive circadian oscillator (MASCO). SCN- and MASCO- (but not FEO-) driven rhythms are progressively disrupted in the R6/2 mouse model of HD. MASCO-driven rhythms are induced by chronic treatment with low dose of methamphetamine and characterised by an increase in period length to greater than 24 h...
December 21, 2017: Neuropharmacology
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