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The adrenergic receptor alpha2C (α2C adrenoceptor), also known as ADRA2C, is one of three highly homologous subtypes of the alpha-2 adrenergic receptors. These G protein-coupled receptors (GPCRs) are critical regulators of neurotransmitter release from sympathetic nerves and central adrenergic neurons. The α2C receptor is primarily localized in the central nervous system, with notable expression in areas such as the midbrain, thalamus, amygdala, and cortex. Upon activation, α2C receptors couple to Gi proteins, inhibiting adenylyl cyclase and reducing cAMP levels, leading to hyperpolarization of neurons and decreased neurotransmitter release. This receptor plays a crucial role in fine-tuning neurotransmission, particularly during low-level neuronal activity, making it a target for drugs affecting mood disorders, cardiovascular function, pain modulation, and sedation/anxiolysis therapies.
Gi-protein mediated inhibition of adenylyl cyclase
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