Receptor Desensitization

Pharmacodynamics

Reduced receptor responsiveness following prolonged or repeated exposure to an agonist. Mechanisms include receptor phosphorylation, internalization, and downregulation. Basis for drug tolerance.

Examples

  • Beta-2 agonist tachyphylaxis
  • Opioid tolerance
  • Nicotinic receptor desensitization

Did You Know?

Reduced receptor responsiveness following prolonged or repeated exposure to an agonist. Mechanisms include receptor phosphorylation, internalization, and downregulation. Basis for drug tolerance.