Spare Receptors

Pharmacodynamics

A concept in receptor pharmacology in which a maximal biological response is achieved when only a fraction of the total receptor population is occupied by agonist. The existence of spare receptors means that the EC50 for the response is lower than the Kd for receptor binding, increasing the sensitivity of the tissue to the agonist. Spare receptor reserves vary by tissue and receptor type.

उदाहरण

  • Acetylcholine at neuromuscular junction: ~80-90% of receptors can be blocked before twitch failure
  • Insulin receptors: maximal glucose uptake at ~5-10% receptor occupancy
  • Opioid receptors in the gut: high receptor reserve contributes to constipation sensitivity

क्या आप जानते हैं?

A concept in receptor pharmacology in which a maximal biological response is achieved when only a fraction of the total receptor population is occupied by agonist. The existence of spare …