Construct · 1 fields · 1 citations

downregulation: a standalone construct

One name. One construct. A landmark on the map.

● anchor · receptors lost on stimulation, one field Nearest construct by meaning·not indexed
downregulation1 CONSTRUCTReceptor downregulationGAVIN · RECEPTOR LOSS

A single standalone construct; nearby constructs are located against it in the Collider. Tap a field for its definition, unit, and measures.

Cellular pharmacology

A cell culls receptors under heavy stimulation

Downregulation is a cell's reduction in the number of a given receptor in response to prolonged or intense stimulation, lowering its future sensitivity to the agonist. Gavin and colleagues' 1974 Insulin-dependent regulation of insulin receptor concentrations gave a direct demonstration in cultured cells, showing insulin itself drives the loss of its own receptors. The referent is a stimulus-driven fall in receptor density (through internalisation and reduced synthesis) that underlies tolerance to many drugs and hormones, the opposite of the receptor increase called upregulation.[1]

Unit
The change (fall) in receptor number per cell after sustained stimulation
Recovery means
Receptor numbers typically recover after the stimulus is withdrawn, as synthesis and recycling restore surface density
Measured by
Quantified by radioligand or antibody binding assays of receptor density before and after prolonged agonist exposure

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Nearby constructs

receptor reserve1 fields · 2 citationsanchor · spare receptors, one fieldtolerance6 fields · 11 citationsjingle · one name, six constructsagonist1 fields · 3 citationsanchor · a standalone construct

References

  1. Gavin, J. R., Roth, J., Neville, D. M., De Meyts, P., & Buell, D. N. (1974). Insulin-dependent regulation of insulin receptor concentrations: A direct demonstration in cell culture. Proceedings of the National Academy of Sciences, 71(1), 84–88. https://doi.org/10.1073/pnas.71.1.84

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