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A M Dygai et al.
Bulletin of experimental biology and medicine, 154(3), 329-333 (2013-03-14)
Using the model of lung fibrosis induced by intratracheal administration of bleomycin we studied anti-fibrotic activity of combined treatment with neuroleptic haloperidol and hyaluronidase immobilized on polyethylene oxide using electron-beam synthesis. It was shown that successive administration of immobilized hyaluronidase
Odrun A Gederaas et al.
Translational oncology, 7(6), 812-823 (2014-12-17)
Non-muscle-invasive bladder cancers (NMIBCs) are tumors confined to the mucosa or the mucosa/submucosa. An important challenge in treatment of NMIBC is both high recurrence and high progression rates. Consequently, more efficacious intravesical treatment regimes are in demand. Inhibition of the
Renee C Gentzel et al.
Neuropharmacology, 99, 256-263 (2015-06-06)
Phosphodiesterase 10A (PDE10A) has garnered attention as a potential therapeutic target for schizophrenia due to its prominent striatal expression and ability to modulate striatal signaling. The present study used the selective PDE10A inhibitor MP-10 and the dopamine D2 antagonist haloperidol
A Angelini et al.
Journal of biological regulators and homeostatic agents, 29(2), 357-365 (2015-07-01)
Multidrug resistance (MDR) mediated by P-glycoprotein (Pgp) remains one of the major obstacles to effective cancer chemotherapy. Several chemosensitizers have been used in vivo and in vitro to reverse MDR but have exhibited several unwanted side effects. Antipsychotics are often
Milena Cannella et al.
Neuropharmacology, 95, 50-58 (2015-03-10)
Neuroadaptive changes involving the indirect pathway of the basal ganglia motor circuit occur in the early phases of parkinsonism. The precise identification of these changes may shed new light into the pathophysiology of parkinsonism and better define the time window
Tatsuya Higashi et al.
Journal of pharmaceutical and biomedical analysis, 117, 155-162 (2015-09-12)
The analysis of changes in the brain neurosteroid (NS) levels due to various stimuli can contribute to the elucidation of their physiological roles, and the discovery and development of new antipsychotic agents targeting neurosteroidogenesis. We developed methods for the differential
Yunbok Kim et al.
Scientific reports, 11(1), 20350-20350 (2021-10-15)
Behaviors driven by intrinsic motivation are critical for development and optimization of physical and brain functions, but their underlying mechanisms are not well studied due to the complexity and autonomy of the behavior. Songbirds, such as zebra finches, offer a
Patrick Oeckl et al.
Experimental neurology, 257, 1-9 (2014-04-22)
The orphan G-protein coupled receptor 6 (GPR6) is a constitutively active receptor which is positively coupled to the formation of cyclic adenosine-3',5'-monophosphate (cAMP). GPR6 is predominantly expressed in striatopallidal neurons. Here, we investigated neurochemical and behavioural effects of Gpr6 deficiency
S Natesan et al.
Translational psychiatry, 4, e376-e376 (2014-04-03)
A number of phosphodiesterase 10A (PDE10) inhibitors are about to undergo clinical evaluation for their efficacy in treating schizophrenia. As phosphodiesterases are in the same signalling pathway as dopamine D2 receptors, it is possible that prior antipsychotic treatment could influence
Ashleigh Pulkoski-Gross et al.
Molecular pharmacology, 87(3), 501-512 (2015-01-02)
Because cancer cell invasion is a critical determinant of metastasis, targeting invasion is a viable approach to prevent metastasis. Utilizing a novel three-dimensional high-throughput invasion assay, we screened a National Cancer Institute compound library and discovered compounds demonstrating inhibitory effects
Samantha L McLean et al.
Journal of pain & palliative care pharmacotherapy, 27(2), 132-135 (2013-05-01)
Nausea and vomiting are common symptoms in palliative care. Haloperidol is often used as an antiemetic in this context, although direct evidence supporting this practice is limited. To evaluate the efficacy and clinical use of haloperidol as an antiemetic in
Limin Shi et al.
Nature communications, 4, 1435-1435 (2013-02-07)
The gut-derived orexigenic peptide hormone ghrelin enhances neuronal firing in the substantia nigra pars compacta, where dopaminergic neurons modulate the function of the nigrostriatal system for motor coordination. Here we describe a novel mechanism by which ghrelin enhances firing of
Priscilla B Pail et al.
Neurotoxicology, 50, 71-80 (2015-08-10)
Mephedrone and methedrone are cathinone-related compounds, which act as non-selective substrates for monoamine transporters, facilitating a neurotransmitter release. We compared the acute pharmacological effects of mephedrone and methedrone, attempting to further evaluate the action mechanisms of methedrone by responsibly and
Ronald J van der Sluis et al.
British journal of pharmacology, 172(9), 2397-2405 (2015-01-13)
Antipsychotic drugs have been shown to modulate the expression of ATP-binding cassette transporter A1 (ABCA1), a key factor in the anti-atherogenic reverse cholesterol transport process, in vitro. Here we evaluated the potential of the typical antipsychotic drug haloperidol to modulate
Susanna Waters et al.
Journal of neural transmission (Vienna, Austria : 1996), 121(11), 1337-1347 (2014-05-13)
The dopaminergic stabilizers pridopidine [4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine] and ordopidine [1-ethyl-4-(2-fluoro-3-(methylsulfonyl)phenyl)piperidine] inhibit psychostimulant-induced hyperactivity, and stimulate behaviour in states of hypoactivity. While both compounds act as dopamine D2 receptor antagonists in vitro, albeit with low affinity, their specific state-dependent behavioural effect profile is
Fabrizio Sanna et al.
Pharmacology, biochemistry, and behavior, 124, 211-219 (2014-06-24)
Outbred Roman high- (RHA) and low-avoidance (RLA) rats, originally selected for rapid vs. poor acquisition of active avoidance in a shuttle box, show differential copulatory patterns when exposed to a receptive female. Indeed, in the first copulation test male RHA
Jie Li et al.
Oncotarget, 5(4), 882-893 (2014-03-25)
Glioblastoma remains one of the deadliest of human cancers, with most patients succumbing to the disease within two years of diagnosis. The available data suggest that simultaneous inactivation of critical nodes within the glioblastoma molecular circuitry will be required for
Cassandra J Bellamy et al.
The Journal of trauma, 66(3), 954-958 (2009-03-12)
Haloperidol, which is commonly used to treat agitation in critically ill patients, has been associated with the development of neuroleptic malignant syndrome (NMS). The purpose of this manuscript was to review the literature describing NMS and haloperidol use in patients
Norma Adán et al.
The Journal of clinical investigation, 123(9), 3902-3913 (2013-08-03)
Chondrocytes are the only cells in cartilage, and their death by apoptosis contributes to cartilage loss in inflammatory joint diseases, such as rheumatoid arthritis (RA). A putative therapeutic intervention for RA is the inhibition of apoptosis-mediated cartilage degradation. The hormone
Hongzhu Li et al.
Experimental cell research, 323(1), 118-130 (2014-01-15)
The physiological and pathological roles of dopamine D2 receptors (DR2) in the regulation of cardiovacular functions have been recognized. DR2 activation protects hypoxia/reoxygenation (H/R)-induced cardiomyocyte injury and apoptosis, and ischemic post-conditioning (PC) plays a critical role in cardioprotection as well;
N Kirk Morton et al.
Journal of psychosocial nursing and mental health services, 51(3), 13-18 (2013-04-03)
Medication nonadherence has been associated with persistence of psychotic symptoms, relapse, and hospitalization in patients with schizophrenia. Patients with untreated psychosis are significantly less likely to achieve remission, whereas antipsychotic drug adherence has been associated with recovery. As such, adherence
Gerard W K Hugenholtz et al.
The Journal of clinical psychiatry, 67(6), 897-903 (2006-07-20)
To determine the doses of haloperidol as a comparator drug in randomized controlled trials (RCTs) with atypical antipsychotics in patients with schizophrenia and to compare these doses with the officially recommended doses for haloperidol in the United States and the
Dan Shan et al.
Schizophrenia research, 144(1-3), 1-8 (2013-01-30)
Glutamate transporters facilitate the buffering, clearance and cycling of glutamate and play an important role in maintaining synaptic and extrasynaptic glutamate levels. Alterations in glutamate transporter expression may lead to abnormal glutamate neurotransmission contributing to the pathophysiology of schizophrenia. In
John P Redrobe et al.
Psychopharmacology, 231(16), 3151-3167 (2014-03-01)
Here, we present the pharmacological characterisation of Lu AF64280, a novel, selective, brain penetrant phosphodiesterase (PDE) 2A inhibitor, in in vitro/in vivo assays indicative of PDE2A inhibition, and in vivo models/assays relevant to cognitive processing or antipsychotic-like activity. The in
Weiqiang Chen et al.
Biochemical and biophysical research communications, 450(1), 55-60 (2014-05-31)
Typical antipsychotics are characterized by extrapyramidal syndrome (EPS). Previous studies demonstrated that typical antipsychotics could inhibit neuronal voltage-gated sodium channel (VGSC). However, EPS typically emerge only upon prolonged exposure. As a result, we examined effects of haloperidol, a prototype typical
Kazuaki Kawaura et al.
Behavioural brain research, 278, 186-192 (2014-10-11)
Glutamatergic dysfunction, particularly the hypofunction of N-methyl-D-aspartate (NMDA) receptors, is involved in the pathophysiology of schizophrenia. The positive modulation of the glycine site on the NMDA receptor has been proposed as a novel therapeutic approach for schizophrenia. However, its efficacy
B Reuss et al.
Journal of molecular neuroscience : MN, 57(1), 123-138 (2015-06-18)
Antibacterial antibodies can cause neurologic side-effects by cross-reactivity with cellular antigens. Here we investigated interactions of antibodies to Neisseria gonorrhoeae (α-NG) - maternal infections by which increases the offspring's risk for later psychosis-with HIBCPP cells, a cell culture model of
Erum Shireen et al.
Pakistan journal of pharmaceutical sciences, 26(2), 271-276 (2013-03-05)
The present study was designed to monitor extrapyramidal symptoms (EPS) elicited by the oral administration of haloperidol at clinically recommended doses and to compare it with EPS produced when the drug is injected intraperitoneally at doses used in animal research.
Chengchun Min et al.
Biochimica et biophysica acta, 1853(1), 41-51 (2014-10-08)
Numerous G protein-coupled receptors (GPCRs) are glycosylated at extracellular regions. The regulatory roles of glycosylation on receptor function vary across receptor types. In this study, we used the dopamine D₂and D₃receptors as an experimental model to understand the underlying principles
A G Pinder et al.
British journal of pharmacology, 157(8), 1523-1530 (2009-07-15)
It is postulated that nitrite requires reduction to nitric oxide in order to exert its relaxant effect upon isolated hypoxic vessels. Herein, we evaluate the relative contribution of nitric oxide and characterize the downstream mechanisms of nitrite-induced vasorelaxation. Aortic rings
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