Published in Neuropharmacology
Neuronal Na+/K+-ATPase is responsible for the maintenance of ionic gradient across plasma membrane. In doing so, in a healthy brain, Na+/K+-ATPase activity accounts for nearly half of total brain energy consumption. The α3-subunit containing Na+/K+-ATPase expression is restricted to neurons. Heterozygous mutations within α3-subunit leads to Rapid-o...
Published in Neuropsychobiology
Background: The results of studies examining the response to experimental pain during the menstrual cycle are conflicting because of differences in the definitions of the menstrual period, outcome measures and types of experimental pain stimulation. So far, there have been only a few studies correlating experimental pain with the levels of gonadal ...
Published in Neuropharmacology
• l -DOPA-induced dyskinesia (LID) develops in many Parkinson's disease patients. • NLX-112 is a highly selective and high efficacy serotonin 5-HT1A receptor agonist. • In MPTP-treated marmosets NLX112 reduced LID without impairing therapeutic activity. • NLX-112 by itself exhibited antiparkinsonian activity (decreased motor disability). • NLX-112 ...
Published in Neuropharmacology
Binding and signaling kinetics have previously proven important in validation of biased agonism at GPCRs. Here we provide a comprehensive kinetic pharmacological comparison of clinically relevant μ-opioid receptor agonists, including the novel biased agonist oliceridine (TRV130) which is in clinical trial for pain management. We demonstrate that th...
Published in Neuropharmacology
There is unmet need to design an analgesic with fewer side effects for severe pain management. Although traditional opioids are the most effective painkillers, they are accompanied by severe adverse responses, such as respiratory depression, constipation symptoms, tolerance, withdrawal, and addiction. We indicated BPR1M97 as a dual mu opioid recept...
Published in Neuropharmacology
Social dysfunction is among the core symptoms of schizophrenia. The neuropeptides oxytocin (OXT) and vasopressin (VP) are involved in the regulation of social behaviour and social cognition. There are indications that both of these neurotransmitter systems are altered in schizophrenia. Prenatal (embryonic day 17) exposure to the neurotoxin methylaz...
Published in Neuropharmacology
The NAD(P)H:quinone oxidoreductase 1 (NQO1) gene encodes a cytosolic flavoenzyme that catalyzes the two-electron reduction of quinones to hydroquinones. A polymorphic form of NQO1 is associated with mood disorders such as schizophrenia. However, the role of NQO1 in dopaminergic system has not yet been elucidated. To determine the role of NQO1 in th...
Published in Neuropharmacology
The underline neuropathology of Parkinson disease is pleiomorphic and its genetic background diverse. Possibly because of this heterogeneity, no effective disease modifying therapy is available. In this paper we give an overview of the genetics of Parkinson disease and explain how this is relevant for the development of new therapies. Copyright © 2...
Published in Neuropharmacology
Glaucoma, the second leading cause of irreversible blindness worldwide, is characterized by the selective death of retinal ganglion cells (RGCs). The group II metabotropic glutamate receptor (mGluR II) activation has been linked to RGC survival, however, the mechanism by which it promotes neuronal survival remains poorly defined. In the present wor...
Published in Neuropharmacology
The neuropeptide hypocretin/orexin plays a broad and important role in physiological functions ranging from addiction, stress, and anxiety to sleep, energy metabolism, and homeostatic regulation. A number of recent reviews addressing the importance of orexin for different addictive behaviors, especially the contribution of orexin-1-receptors (Ox1Rs...
