In ischemic stroke, there is only one approved drug, tissue plasminogen activator, to be used in clinical conditions for thrombolysis. New neuroprotective therapies for ischemic stroke are desperately needed. Several targets and pathways have been shown to confer neuroprotective effects in ischemic stroke. G-protein-coupled receptors (GPCRs) are one of the most frequently targeted receptors for developing novel therapeutics for central nervous system disorders. GPCRs are a large family of cell surface receptors that response to a wide variety of extracellular stimuli. GPCRs are involved in a wide range of physiological and pathological processes. More than 90% of the identified non-sensory GPCRs are expressed in the brain, where they play important roles in regulating mood, pain, vision, immune responses, cognition, and synaptic transmission. There is also good evidence that GPCRs are implicated in the pathogenesis of stroke. This review narrates the pathophysiological role and possible targeted therapy of GPCRs in ischemic stroke.
