Regulation of receptors involves upregulation or downregulation, affecting drug sensitivity and therapeutic response.
Regulation of Receptors
- Cells dynamically regulate receptors in response to various stimuli to maintain homeostasis.
Key mechanisms include:
Receptors can change in number or sensitivity in response to drug exposure:
-
Upregulation
- Increase in receptor number or sensitivity.
- Occurs after prolonged use of antagonists or loss of endogenous ligand.
- Example: Sudden withdrawal of β-blockers → hypersensitive response.
-
Downregulation
- Decrease in receptor number or sensitivity.
- Caused by prolonged exposure to agonists.
- Example: Continuous use of salbutamol (β2 agonist) → tolerance.
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