Sensory neuron-specific receptor activation elicits central and peripheral nociceptive effects in rats.

摘要: The sensory neuron-specific G protein coupled receptors (SNSRs) have been described as a family of whose expression in small diameter neurons the trigeminal and dorsal root ganglia suggests an implication nociception. To date, physiological function(s) SNSRs remain unknown. Hence, aim present study was to determine effects rat SNSR1 activation on nociception rats. pharmacological characterization initially performed vitro identify specific ligand, which could be used subsequently for testing. Among all ligands tested, γ2-MSH most potent at activating SNSR1. Structure–activity relationship studies revealed that active moiety recognized by C-terminal part γ2-MSH. radiolabeled γ2-MSH, γ2-MSH-6–12, bound with high affinity membranes derived from skin spinal cord, demonstrating presence receptor both proximal distal terminals ganglia. investigate role SNSR, were tested behavioral assays pain sensitivity Selective agonists produced spontaneous behavior, enhanced heat mechanical when injected intradermally, hypersensitivity centrally, consistent localization central peripheral sites. Together, these results clearly indicate plays may provide novel therapeutic opportunities analgesia.