Receptor Upregulation
An increase in the number or sensitivity of receptors on the cell surface, usually in response to chronic antagonist exposure or reduced agonist stimulation. Upregulation is a compensatory mechanism that can lead to rebound effects upon abrupt drug withdrawal. It represents an important consideration for tapering schedules.
Exemples
- Beta-receptor upregulation after chronic propranolol — rebound tachycardia on withdrawal
- D2 receptor upregulation after long-term antipsychotic use — tardive dyskinesia risk
- GABA-A receptor upregulation concept in benzodiazepine withdrawal seizures
Le saviez-vous ?
An increase in the number or sensitivity of receptors on the cell surface, usually in response to chronic antagonist exposure or reduced agonist stimulation. Upregulation is a compensatory mechanism that …