The adaptive increase in the density or sensitivity of specific receptor proteins on the surface of neurons, resulting in an enhanced responsiveness to their corresponding neurotransmitter molecules. This upregulation is a therapeutic goal in conditions associated with low neurotransmitter activity or receptor desensitization, aiming to improve synaptic efficiency and signal transduction. It is a fundamental mechanism for restoring optimal neurological and psychological function.
Origin
This term is rooted in molecular neurobiology and pharmacology, describing a key mechanism of neuronal plasticity. ‘Neurotransmitter receptor’ refers to the protein that binds the signaling molecule, and ‘upregulation’ describes the homeostatic increase in the number of these receptors. This phenomenon is often a compensatory response to chronic low-level stimulation.
Mechanism
Upregulation is primarily regulated at the gene expression level, where a cell increases the transcription and translation of the receptor protein’s genetic code. This can be induced by temporarily reducing the presence of the stimulating neurotransmitter or by providing specific cofactors and membrane-building blocks to facilitate receptor insertion into the postsynaptic membrane. The resulting increased receptor availability amplifies the signal received by the neuron, improving communication across the synapse.
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