Topic: G-protein-coupled receptors

Cannabidiol (CBD) is a phytocannabinoid with potential as a therapy for a variety of diseases. CBD may act via cannabinoid receptors but also via other G-protein-coupled receptors (GPCRs), including the adenosine A2A receptor. Homogenous binding and signaling assays in Chinese hamster ovary (CHO) cells expressing the human version of the A2A receptor were performed to address the effect of CBD on receptor functionality. CBD was not able to compete for the binding of a SCH 442416 derivative labeled with a red emitting fluorescent probe that is a selective antagonist that binds to the orthosteri

Norepinephrine (NE) is one of the main neuromodulators in the brain influencing a plethora of behavioral outputs including both autonomic and cognitive functions, such as emotional learning and stress responses, through a brain-wide network of projections emanating from the Locus Coeruleus (LC). Genetically encoded indicators engineered from G-protein-coupled receptors (GPCRs) have been proven essential tools for neuroscience enabling in vivo imaging of neuromodulators with high spatiotemporal resolution. Current state-of-the-art NE sensors allow for in vivo optical detection of NE, however, t

Astrocytes are the most abundant glial cell type in the central nervous system. They express G-protein-coupled receptors (GPCRs), which respond to inflammatory and stress mediators. Activation of astrocytic GPCRs triggers elevation in intracellular calcium levels and the production and release of astrocytic factors. These astrocytic factors play crucial roles in modulating synapse numbers and synaptic plasticity.Changes in synapse numbers have been documented in neurodevelopmental disorders (NDDs). Many epidemiological studies indicate that chronic inflammation and stress during critical neuro

The primary cilium, a microtubule-based organelle that extends into the extracellular space, plays a crucial role in signal transduction. It acts as an 'antenna' for signal conversion through different pathways, containing various types of proteins, such as G-protein-coupled receptors (GPCRs). Notably, it is involved in the regulation of glucose homeostasis, a vital process for cellular function and energy balance, which includes glucose detection associated with both metabolic (GLUTs and glucokinase) and independent mechanisms. Sweet taste receptors (STR), which are GPCRs composed of subunits