Search results for "suppression [background]"
showing 10 items of 11 documents
Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake
2017
The extracellular effects of the endocannabinoids anandamide and 2-arachidonoyl glycerol are terminated by enzymatic hydrolysis after crossing cellular membranes by facilitated diffusion. The lack of potent and selective inhibitors for endocannabinoid transport has prevented the molecular characterization of this process, thus hindering its biochemical investigation and pharmacological exploitation. Here, we report the design, chemical synthesis, and biological profiling of natural product-derived N-substituted 2,4-dodecadienamides as a selective endocannabinoid uptake inhibitor. The highly potent (IC50 = 10 nM) inhibitor N-(3,4-dimethoxyphenyl)ethyl amide (WOBE437) exerted pronounced canna…
Anxiety, Stress, and Fear Response in Mice With Reduced Endocannabinoid Levels
2016
Abstract Background Disruption of the endocannabinoid system through pharmacological or genetic invalidation of cannabinoid CB 1 receptors has been linked to depression in humans and depression-like behaviors in mice. The two main endogenous cannabinoids, anandamide and 2-arachidonoyl glycerol (2-AG), are produced on demand from phospholipids. The pathways and enzymes involved in endocannabinoid biosynthesis thus play a major role in regulating the activity of this system. This study investigates the role of the main 2-AG producing enzyme diacylglycerol lipase α (DAGL-α). Methods We generated and used knockout mice lacking DAGL-α ( Dagla −/− ) to assess the behavioral consequences of reduce…
Cannabinoid CB1 receptor activation modulates spontaneous contractile activity in mouse ileal longitudinal muscle.
2007
The purpose of the present study was to examine whether cannabinoid receptor agonists influence spontaneous contractile activity of longitudinal muscle in mouse ileum in vitro. Isolated segments of mouse ileum displayed spontaneous contractions with an amplitude and frequency of about 300 mg and 30 cpm, respectively. The endocannabinoid anandamide (1-100 microM), the selective cannabinoid CB(1) receptor agonist, ACEA (0.1 microM-10 microM), but not the selective cannabinoid CB(2) receptor agonist, JWH 133 (0.1 microM-10 microM), reduced in a concentration-dependent manner the spontaneous mechanical activity. The inhibitory effect consisted in a decrease of the mean amplitude of longitudinal…
Vehicle localization based on scene perception
2021
The vision-based vehicle localization task is tackled as an image-based place recognition problem in this thesis. As image representation is an important process to place recognition, we proposed place recognition methods focusing on increasing the quality of image features. First, the dynamic object removal step is proposed to remove the dynamic objects, such as vehicles and pedestrians, of an image by semantic segmentation method and restore their background information by image inpainting method. Second, reducing instead of removing the noisy information of an image is proposed. Using the image blurring method to reduce the image noise, the performance of place recognition is improved wi…
Immunosuppression Drugs Seize the Overacting Immune System by Preventing the Cytokine Storm In COVID-19 Symptoms
2021
The COVID-19 over-active other diseases within the human body especially respiratory system in which cytokine storm abnormally developed that results in the excessive killing of cells within the autoimmune system. To resolve this major issue, a systematic review paper is developed whose major aim is to propose such immunosuppression drugs that can easily seize the overacted immune system by blocking the cytokine storm action within human body, by systematically overview the previous scholars' articles, case reports and authentic websites based valid data. To justify this aim, different latest and authentic medicine's journals and papers are collected by posting four major keywords like "Cyt…
Inhibition by Anandamide and Synthetic Cannabimimetics of the Release of [3H]d-Aspartate and [3H]GABA from Synaptosomes Isolated from the Rat Hippoca…
2004
Cannabinoids (CB) can act as retrograde synaptic mediators of depolarization-induced suppression of inhibition or excitation in hippocampus. This mechanism may underlie the impairment of some cognitive processes produced by these compounds, including short-term memory formation in the hippocampus. In this study, we investigated several compounds known to interact with CB receptors, evaluating their effects on K +-evoked release of [ 3H]d-aspartate ([ 3H]d-ASP) and [ 3H]GABA from superfused synaptosomes isolated from the rat hippocampus. [ 3H]d-ASP and [ 3H]GABA release were inhibited to different degrees by the synthetic cannabinoids WIN 55,212-2; CP 55,940, and arachidonyl-2′- chloroethyla…
A runner’s high depends on cannabinoid receptors in mice
2015
Exercise is rewarding, and long-distance runners have described a runner's high as a sudden pleasant feeling of euphoria, anxiolysis, sedation, and analgesia. A popular belief has been that endogenous endorphins mediate these beneficial effects. However, running exercise increases blood levels of both β-endorphin (an opioid) and anandamide (an endocannabinoid). Using a combination of pharmacologic, molecular genetic, and behavioral studies in mice, we demonstrate that cannabinoid receptors mediate acute anxiolysis and analgesia after running. We show that anxiolysis depends on intact cannabinoid receptor 1 (CB1) receptors on forebrain GABAergic neurons and pain reduction on activation of pe…
Le retour au droit de retour légal de l'ascendant donateur ?
2006
International audience
Nitrogen uptake and nitrogen fertilizer recovery in old and modern wheat genotypes grown in the presence or absence of interspecific competition
2015
Choosing genotypes with a high capacity for taking up nitrogen (N) from the soil and the ability to efficiently compete with weeds for this nutrient is essential to increasing the sustainability of cropping systems that are less dependent on auxiliary inputs. This research aimed to verify whether differences exist in N uptake and N fertilizer recovery capacity among wheat genotypes and, if so, whether these differences are related to a different competitive ability against weeds of wheat genotypes. To this end, 12 genotypes, varying widely in morphological traits and year of release, were grown in the presence or absence of interspecific competition (using Avena sativa L. as a surrogate wee…
Endocannabinoid Role in Synaptic Plasticity and Learning
2009
Endocannabinoids have recently emerged as versatile modulators of synaptic transmission and can act as retrograde neurotransmitters. As they cannot be stored in synaptic vesicles, endocannabinoid signaling is believed to start ‘on-demand,’ via a stimulus-dependent synthesis from membranous precursors at the postsynaptic site. After synthesis, endocannabinoids bind presynaptically to cannabinoid type 1 (CB1) receptors, leading to a short- or long-term suppression of neurotransmitter release. CB1 receptors are present in a plethora of different synaptic connections in the brain. Electrophysiological and behavioral analyses of mutant mice lacking CB1 receptors and of pharmacologically treated …