The lactate receptor, G‐protein‐coupled receptor 81/hydroxycarboxylic acid receptor 1: Expression and action in brain

摘要: We have proposed that lactate is a "volume transmitter" in the brain and underpinned this by showing receptor, G-protein-coupled receptor 81 (GPR81, also known as HCA1 or HCAR1), which promotes lipid storage adipocytes, active mammalian brain. This includes cerebral neocortex hippocampus, where it can be stimulated physiological concentrations of HCAR1 agonist 3,5-dihydroxybenzoate to reduce cAMP levels. Cerebral concentrated on postsynaptic membranes excitatory synapses enriched at blood-brain barrier. In synaptic spines immunoreactivity located subplasmalemmal vesicular organelles, suggesting trafficking from plasma membrane. Through activation HCAR1, act volume transmitter links neuronal activity, blood flow, energy metabolism, substrate availability, including glucose- glycogen-saving response. may contribute optimizing concentration. For instance, prefrontal cortex, excessively high levels are implicated impaired cognition old age, fatigue, stress, schizophrenia deposition phosphorylated tau protein Alzheimer's disease. could serve ameliorate these conditions might through downstream mechanisms other than cAMP. Lactate exits cells monocarboxylate transporters an equilibrating manner astrocyte anion channels activated depolarization. addition locally produced lactate, exercising muscle well exogenous agonists, e.g., fruits berries, activate vessels cells.