Regulation of Receptors

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:

Regulation of Receptors

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  1. 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.
  2. 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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