Cause of Receptor Down-Regulation
Down-regulation of receptors is caused by:
- Enzyme inhibition
- First-pass metabolism
- Continuous agonist exposure — Correct Answer
- Prolonged antagonist exposure
Correct Answer: Continuous exposure to an agonist
When tissues are continuously exposed to an agonist, the number of receptors decreases — this is called down-regulation. It is a reason for tachyphylaxis (decreased response on repeated administration).
Contrast: Up-Regulation
Prolonged contact with an antagonist leads to formation of new receptors — this is called up-regulation. This explains why sudden withdrawal of an antagonist (e.g. propranolol) can lead to rebound effects.
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