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dopamine 5 receptor

Cameron W Morris, Darryl S Watkins, Asma B Salek, Michael C Edler, Anthony J Baucum
Spinophilin is the most abundant protein phosphatase 1 targeting protein in the postsynaptic density of dendritic spines. Spinophilin associates with myriad synaptic proteins to regulate normal synaptic communication; however, the full complement of spinophilin interacting proteins and mechanisms regulating spinophilin interactions are unclear. Here we validate an association between spinophilin and the scaffolding protein, disks large-associated protein 3 (SAP90/PSD-95 associated protein 3; SAPAP3). Loss of SAPAP3 leads to obsessive-compulsive disorder (OCD)-like behaviors due to alterations in metabotropic glutamate receptor (mGluR) signaling...
June 13, 2018: Molecular and Cellular Neurosciences
Wei Zheng, Dong-Bin Cai, Xin-Hu Yang, Lu Li, Qing-E Zhang, Chee H Ng, Gabor S Ungvari, Xian-Bin Li, Yu-Ping Ning, Yu-Tao Xiang
BACKGROUND: Lurasidone, an azapirone derivative, is a novel second generation antipsychotic with potent binding affinity for dopamine D2, serotonin 5-HT2A , 5-HT7, 5-HT1A, and noradrenaline alpha2C receptors. This updated meta-analysis of randomized controlled trials (RCTs) examined the short-term efficacy and tolerability of lurasidone in the treatment of acute schizophrenia. METHODS: Double-blinded RCTs reporting on the short-term effects of lurasidone were included...
June 5, 2018: Journal of Psychiatric Research
Lucia Recinella, Annalisa Chiavaroli, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Marilisa Pia Dimmito, Szabolcs Dvorácskó, Csaba Tömböly, Luigi Brunetti, Giustino Orlando, Sheila Leone
BACKGROUND: The endocannabinoid (eCB) system is strongly involved in the regulation of anxiety and feeding behavior. RVD-hemopressin(α) [RVD-hp(α)], a N-terminally extended form of hemopressin, is a negative allosteric modulator of the cannabinoid (CB) 1 receptor and a positive allosteric modulator of CB2 receptor which has been recently reported to exert anxiolytic/antidepressant and anorexigenic effects after peripheral administration in rats. Pharmacological evidences reported a possible link between brain hypocretin/orexin, monoamine and eCB systems, as regards appetite and emotional behavior control...
February 2, 2018: Pharmacological Reports: PR
Huamin Xu, Xiaodong Liu, Jianjian Xia, Tianshu Yu, Yanan Qu, Hong Jiang, Junxia Xie
Increasing evidence has confirmed that nigral iron accumulation and activation of NMDA receptors (NRs) contribute to the neurodegeneration of dopamine (DA) neurons in Parkinson's disease (PD). Earlier work indicated that activation of NRs participated in iron metabolism in the hippocampus. However, the relationship between activation of NRs and iron accumulation in DA neurons of the substantia nigra in PD was unknown. In this study, our results showed that NRs inhibitors MK-801 and AP5 protected nigrostriatal projection system and reduced nigral iron levels of 6-hydroxydopamine (6-OHDA)-induced PD rats...
June 13, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
Ma Ludivina Robles-Osorio, Renata García-Franco, Carlos D Núñez-Amaro, Ximena Mira-Lorenzo, Paulina Ramírez-Neria, Wendy Hernández, Ellery López-Star, Thomas Bertsch, Gonzalo Martínez de la Escalera, Jakob Triebel, Carmen Clapp
Background: Diabetic retinopathy (DR) and diabetic macular edema (DME) are potentially blinding, microvascular retinal diseases in people with diabetes mellitus. Preclinical studies support a protective role of the hormone prolactin (PRL) due to its ocular incorporation and conversion to vasoinhibins, a family of PRL fragments that inhibit ischemia-induced retinal angiogenesis and diabetes-derived retinal vasopermeability. Here, we describe the protocol of an ongoing clinical trial investigating a new therapy for DR and DME based on elevating the circulating levels of PRL with the prokinetic, dopamine D2 receptor blocker, levosulpiride...
2018: Frontiers in Endocrinology
Harumasa Takano
Positron emission tomography (PET) is a non-invasive imaging technique used to assess various brain functions, including cerebral blood flow, glucose metabolism, and neurotransmission, in the living human brain. In particular, neurotransmission mediated by the monoamine neurotransmitters dopamine, serotonin, and norepinephrine, has been extensively examined using PET probes, which specifically bind to the monoamine receptors and transporters. This useful tool has revealed the pathophysiology of various psychiatric disorders, including schizophrenia, and the mechanisms of action of psychotropic drugs...
2018: Frontiers in Psychiatry
Lionel Froux, Morgane Le Bon-Jego, Cristina Miguelez, Elisabeth Normand, Stephanie Morin, Stéphanie Fioramonti, Massimo Barresi, Andreas Frick, Jerome Baufreton, Anne Taupignon
Corticofugal fibers target the subthalamic nucleus (STN), a component nucleus of the basal ganglia, in addition to the striatum, their main input. The cortico-subthalamic, or hyperdirect, pathway, is thought to supplement the cortico-striatal pathways in order to interrupt/change planned actions. To explore the previously unknown properties of the neurons that project to the STN, retrograde and anterograde tools were used to specifically identify them in the motor cortex and selectively stimulate their synapses in the STN...
June 11, 2018: Scientific Reports
Juan Camilo Jurado-Coronel, Alix E Loaiza, John E Díaz, Ricardo Cabezas, Ghulam Md Ashraf, Amirhossein Sahebkar, Valentina Echeverria, Janneth González, George E Barreto
Parkinson's disease (PD) is a neurodegenerative pathology characterized by resting tremor, rigidity, bradykinesia, and loss of dopamine-producing neurons in the pars compacta of the substantia nigra in the central nervous system (CNS) that result in dopamine depletion in the striatum. Oxidative stress has been documented as a key pathological mechanism for PD. Epidemiological studies have shown that smokers have a lower incidence of PD. In this aspect, different studies have shown that nicotine, a chemical compound found in cigarette, is capable of exerting beneficial effects in PD patients, but it can hardly be used as a therapeutic agent because of its inherent toxicity...
June 7, 2018: Molecular Neurobiology
Ali Ghanbari, Nasroallah Moradi Kor, Ali Rashidy-Pour
Previous studies have shown that the neuropeptide bombesin (BBS) enhances consolidation of specifically for inhibitory avoidance memory in adult rats. However, its effect on memory consolidation during premature period is not clear as well. Thus, this study evaluated the effect of BBS and its interaction with glutamatergic and dopaminergic systems on memory consolidation in rat pups. Male and female rat pups (30 days old) were trained in an inhibitory avoidance (IA) task (0.5 mA, 3 s footshock). Memory retention was tested 24 h later during which the latency to re-enter to the shock compartment was recorded...
June 1, 2018: Neuropeptides
Asaka Sato, Yasushi Hara
PURPOSE: To evaluate the protein expression of somatostatin receptor (SSTR) 2, SSTR5 and dopamine D2 receptor (DA2R)-targets of somatostatin analogs and dopamine agonists-in normal canine pituitary and canine adrenocorticotropic hormone (ACTH)-secreting pituitary adenomas. METHODS: Six normal canine pituitary glands and 14 canine ACTH-secreting pituitary adenoma cases were included in this study. The protein expression of SSTR2, SSTR5 and DA2R was determined by double-label immunofluorescence staining of these receptors and ACTH...
May 4, 2018: Research in Veterinary Science
Xiting Zhang, Lin Li, Ting Chen, Zuoyan Sun, Weiwei Tang, Shuang Wang, Tianqi Wang, Yi Wang, Han Zhang
Tonic traditional Chinese medicine is widely used in clinical practice and is categorized into four main drugs, namely, Qi-supplementing, Blood-enriching, Yin-nourishing, and Yang-tonifying. Neurotransmitters play a coordinating role in the nervous system, visceral function, and stress response. The excitation or suppression of the central nervous system is closely related to various diseases, such as insomnia, depression, Alzheimer's disease, Parkinson's disease, and perimenopausal syndrome. An increasing amount of evidence shows that Chinese tonic herb and its active ingredients can delay the occurrence and development of these diseases by modulating related neurotransmitters and their receptors, including norepinephrine (NE), serotonin (5-HT), dopamine (DA), acetylcholine (ACh), and γ -aminobutyric acid (GABA)...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
K V Derkach, I B Sukhov, V M Bondareva, A O Shpakov
Metformin (MF), a first-line drug in the treatment of diabetes mellitus, has been used in the recent years to treat obesity. Its therapeutic effect is due not only to the influence on the peripheral tissues, but also on the hypothalamus, which controls food behavior and energy metabolism. The aim was to study the effect of MF therapy (200 mg/kg/day, 8 weeks) in rats with obesity caused by a high-carbohydrate/high-fat diet on the metabolic and hormonal parameters and functional state of the hypothalamic signaling systems...
2018: Advances in Gerontology, Uspekhi Gerontologii
Guofang Shen, Feng Han, Wei-Xing Shi
Indirect evidence suggests that low doses of ketamine disinhibit (excite) pyramidal neurons in the prefrontal cortex (PFC). In this study, we directly examined the effect of ketamine on PFC pyramidal neurons using simultaneous single-cell and local-field-potential (LFP) recording in chloral hydrate-anesthetized rats. In all animals studied, PFC LFPs showed oscillations (0.3-1.5 Hz) between the active UP state and the relatively quiescent DOWN state, and pyramidal neurons fired preferentially during the UP state...
May 31, 2018: Neuroscience
Glaucia Tobaldini, Natalia F Sardi, Vinicius A Guilhen, Luana Fischer
The ability to modulate pain perception is as critical to survival as pain itself. The most known pain modulation pathway is the PAG-RVM (periaqueductal gray-rostral ventromedial medulla) descending system. In this study, we hypothesized that it is functionally linked to the ascending nociceptive control, which is a form of pain-induced analgesia dependent on mesolimbic mechanisms. To test this hypothesis, we used a pharmacological approach, in which the antinociception induced by noxious stimulation (forepaw injection of capsaicin) was detected in a standard rat model of inflammatory pain (hindpaw injection of carrageenan)...
June 1, 2018: Molecular Neurobiology
Nako Nakatsuka, Huan H Cao, Stephanie Deshayes, Arin Lucy Melkonian, Andrea M Kasko, Paul S Weiss, Anne M Andrews
Aptamers are chemically synthesized oligonucleotides or peptides with molecular recognition capabilities. We investigated recognition of substrate-tethered small-molecule targets, using neurotransmitters as examples, and fluorescently labeled DNA aptamers. Substrate regions patterned via microfluidic channels with dopamine or L-tryptophan were selectively recognized by previously identified dopamine or L-tryptophan aptamers, respectively. The on-substrate dissociation constant determined for the dopamine aptamer was comparable to, though slightly greater than the previously determined solution dissociation constant...
May 31, 2018: ACS Applied Materials & Interfaces
Dino Luethi, Matthias E Liechti
Background: Pharmacological profiles of new psychoactive substances (NPSs) can be established rapidly in vitro and provide information on potential psychoactive effects in humans. The present study investigated whether specific in vitro monoamine transporter and receptor interactions can predict effective psychoactive doses in humans. Methods: We correlated previously assessed in vitro data of stimulants and psychedelics with human doses that are reported on the Internet and in books...
May 29, 2018: International Journal of Neuropsychopharmacology
Arun Parashar, Vineet Mehta, Udayabanu Malairaman
Objective: Diabetic neuropathy is a chronic and often disabling condition that affects a significant number of individuals with diabetes mellitus (DM). It is now established that DM causes various CNS complications like Alzheimer's, dementia, anxiety, depression, neurodegeneration, mood disorders, cognitive dysfunctioning, and so on. Since amygdala and dopaminergic circuitry are critical in controlling several aspects of social behavior, even social recognition memory (SRM), we aimed to study the expression analysis of dopaminergic circuitry in amygdala using real-time polymerase chain reaction...
May 2018: Annals of Neurosciences
Rita Khoury, Noam Grysman, Jake Gold, Kush Patel, George T Grossberg
Despite recent advances in Alzheimer's disease (AD) research, no breakthrough treatments have been discovered. Cholinesterase inhibitors and the NMDA-receptor antagonist memantine are currently the two approved symptomatic treatments for AD. 5HT-6 receptor antagonism has recently emerged as a promising treatment strategy to improve cognition in AD, with a modest side effect profile. Areas Covered: 5-HT6 receptors, exclusively found in the central nervous system, modulate primarily GABA and glutamate levels, facilitating the secondary release of other neurotransmitters including dopamine, noradrenaline and acetylcholine, all of which are compromised in AD...
May 31, 2018: Expert Opinion on Investigational Drugs
Furong Huang, Lishuai Zhang, Qiongsi Wang, Yanan Yang, Qihang Li, Yi Wu, Jiangfan Chen, Jia Qu, Xiangtian Zhou
Purpose: To determine the roles of dopamine D2 receptors (D2Rs) and dopamine D1 receptors (D1Rs) in the inhibition of form-deprivation myopia (FDM) by the nonselective dopamine agonist apomorphine (APO) in D2R-knockout (D2R-KO) and D1R-KO mice. Methods: Retinal layer thicknesses and electroretinograms (ERGs) were analyzed in KO mice and in D2R and D1R antagonist-treated mice. D2R-KO or D1R-KO mice and wild-type (WT) littermates were subjected to form deprivation during postnatal weeks 5 to 8...
May 1, 2018: Investigative Ophthalmology & Visual Science
Gregory L Powell, John Paul Bonadonna, Annika Vannan, Kuiying Xu, Robert H Mach, Robert R Luedtke, Janet L Neisewander
AIMS: The dopamine D3 receptor (D3R) is a pharmacotherapeutic target for drug dependence. We have successfully imaged human D3Rs using radiolabeled LS-3-134, an arylamide phenylpiperazine with moderate selectivity for the D3R over D2R and low efficacy at the D2 and D3R. In this study, we screened for effects of LS-3-134 as a potential anti-cocaine therapeutic. METHODS: Male rats were pretreated with LS-3-134 (0, 1.0, 3.2, or 5.6 mg/kg, IP) 15 min prior to tests for its effects on spontaneous and cocaine-induced locomotion...
May 25, 2018: Pharmacology, Biochemistry, and Behavior
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