What is upregulation and downregulation of receptors?

What is upregulation and downregulation of receptors?

What is upregulation and downregulation of receptors?

A mechanism for the increased or decreased sensitivity to agonists and antagonist drugs suggests that decreased exposure to an agonist results in an increase in the number of receptors (upregulation), while increased exposure to an agonist can result in a decrease in the number of receptors (downregulation).

When do receptors need to be up or down regulated?

  • Receptors are created, or expressed by the DNA of the cell, and they can be increased or up regulated when the signal is weak, or decreased/down regulated, when it is strong. Up regulation involves increase in the number of receptors due to external stimulation.

What happens to receptors when a drug is discontinued?

  • Downregulation and upregulation of receptors. The disequilibrium caused by these changes often causes withdrawal when the long-term use of a drug is discontinued. However, the use of certain receptor antagonists may also damage receptors faster than they upregulate (internalization of receptors due to antagonism).

What causes an increase in the number of receptors?

  • Together, PPARa and GR stimulation result in an enhanced response. Upregulation Upregulation refers to an increase in the number of receptors due to prolonged deprivation of receptors of interacting with their physiological neurotransmitter (e.g. by denervation of chronic use of a receptor antagonist).

What are the effects of Alpha 2 agonists?

  • Alpha-2 agonist agents cause neuromodulation in these centers, leading to sedation, analgesia, vasodilatation, and bradycardia with little effect on the respiratory drive, which accounts for their good safety profile. The 2 major drugs in this group are clonidine and dexmedetomidine.

Related Posts: