
The discovery of a G-protein-coupled receptor for lactate named hydroxycarboxylic acid receptor 1 (HCAR1) in neurons has pointed to additional nonmetabolic effects of lactate for regulating neuronal network activity. In this study, we characterized the intracellular pathways engaged by HCAR1 activation, using mouse primary cortical neurons from wild-type (WT) and HCAR1 knock-out (KO) mice from both sexes. Using whole-cell patch clamp, we found that the activation of HCAR1 with 3-chloro-5-hydroxybenzoic acid (3Cl-HBA) decreased miniature EPSC frequency, increased paired-pulse ratio, decreased firing frequency, and modulated membrane intrinsic properties. Using fast calcium imaging, we show that HCAR1 agonists 3,5-dihydroxybenzoic acid, 3Cl-HBA, and lactate decreased by 40% spontaneous calcium spiking activity of primary cortical neurons from WT but not from HCAR1 KO mice. Notably, in neurons lacking HCAR1, the basal activity was increased compared with WT. HCAR1 mediates its effect in neurons through a Giα-protein. We observed that the adenylyl cyclase-cAMP-protein kinase A axis is involved in HCAR1 downmodulation of neuronal activity. We found that HCAR1 interacts with adenosine A1, GABAB, and α2A-adrenergic receptors, through a mechanism involving both its Giα and Giβγ subunits, resulting in a complex modulation of neuronal network activity. We conclude that HCAR1 activation in neurons causes a downmodulation of neuronal activity through presynaptic mechanisms and by reducing neuronal excitability. HCAR1 activation engages both Giα and Giβγ intracellular pathways to functionally interact with other Gi-coupled receptors for the fine tuning of neuronal activity.SIGNIFICANCE STATEMENT Expression of the lactate receptor hydroxycarboxylic acid receptor 1 (HCAR1) was recently described in neurons. Here, we describe the physiological role of this G-protein-coupled receptor (GPCR) and its activation in neurons, providing information on its expression and mechanism of action. We dissected out the intracellular pathway through which HCAR1 activation tunes down neuronal network activity. For the first time, we provide evidence for the functional cross talk of HCAR1 with other GPCRs, such as GABAB, adenosine A1- and α2A-adrenergic receptors. These results set HCAR1 as a new player for the regulation of neuronal network activity acting in concert with other established receptors. Thus, HCAR1 represents a novel therapeutic target for pathologies characterized by network hyperexcitability dysfunction, such as epilepsy.
Cerebral Cortex, Male, Mice, Knockout, Neurons, Miniature Postsynaptic Potentials, Primary Cell Culture, Action Potentials, Excitatory Postsynaptic Potentials, Nerve Tissue Proteins, Heterotrimeric GTP-Binding Proteins, Second Messenger Systems, Receptors, G-Protein-Coupled, Mice, Inbred C57BL, Mice, Cyclic AMP, Lactates, Animals, Female, Calcium Signaling, Cells, Cultured, Action Potentials; Animals; Calcium Signaling/drug effects; Cells, Cultured; Cerebral Cortex/cytology; Cyclic AMP/physiology; Excitatory Postsynaptic Potentials/drug effects; Excitatory Postsynaptic Potentials/physiology; Female; Heterotrimeric GTP-Binding Proteins/physiology; Lactates/metabolism; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Miniature Postsynaptic Potentials/drug effects; Miniature Postsynaptic Potentials/physiology; Nerve Tissue Proteins/agonists; Nerve Tissue Proteins/deficiency; Nerve Tissue Proteins/genetics; Nerve Tissue Proteins/physiology; Neurons/drug effects; Neurons/physiology; Primary Cell Culture; Receptors, G-Protein-Coupled/agonists; Receptors, G-Protein-Coupled/deficiency; Receptors, G-Protein-Coupled/genetics; Receptors, G-Protein-Coupled/physiology; Second Messenger Systems/drug effects; GPR81; HCAR1; intracellular pathway; lactate; neurons; spontaneous activity
Cerebral Cortex, Male, Mice, Knockout, Neurons, Miniature Postsynaptic Potentials, Primary Cell Culture, Action Potentials, Excitatory Postsynaptic Potentials, Nerve Tissue Proteins, Heterotrimeric GTP-Binding Proteins, Second Messenger Systems, Receptors, G-Protein-Coupled, Mice, Inbred C57BL, Mice, Cyclic AMP, Lactates, Animals, Female, Calcium Signaling, Cells, Cultured, Action Potentials; Animals; Calcium Signaling/drug effects; Cells, Cultured; Cerebral Cortex/cytology; Cyclic AMP/physiology; Excitatory Postsynaptic Potentials/drug effects; Excitatory Postsynaptic Potentials/physiology; Female; Heterotrimeric GTP-Binding Proteins/physiology; Lactates/metabolism; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Miniature Postsynaptic Potentials/drug effects; Miniature Postsynaptic Potentials/physiology; Nerve Tissue Proteins/agonists; Nerve Tissue Proteins/deficiency; Nerve Tissue Proteins/genetics; Nerve Tissue Proteins/physiology; Neurons/drug effects; Neurons/physiology; Primary Cell Culture; Receptors, G-Protein-Coupled/agonists; Receptors, G-Protein-Coupled/deficiency; Receptors, G-Protein-Coupled/genetics; Receptors, G-Protein-Coupled/physiology; Second Messenger Systems/drug effects; GPR81; HCAR1; intracellular pathway; lactate; neurons; spontaneous activity
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