Enkephalinase

Enkephalinase, also known as neutral endopeptidase (NEP), is an enzyme that plays a crucial role in the regulation of various physiological processes in the human body. This article will provide an overview of enkephalinase, its functions, and its significance in different systems.

Overview

Enkephalinase is a type of peptidase enzyme that belongs to the metalloprotease family. It is primarily found in the central nervous system (CNS), as well as in peripheral tissues such as the kidneys, lungs, and intestines. Enkephalinase is responsible for the degradation of enkephalins, which are endogenous opioid peptides involved in pain modulation, mood regulation, and other physiological functions.

Functions

Enkephalinase plays a crucial role in the regulation of pain perception. Enkephalins, which are produced in response to painful stimuli, bind to opioid receptors in the CNS, leading to analgesic effects. However, the activity of enkephalinase limits the duration of these effects by breaking down enkephalins into inactive fragments. By regulating the levels of enkephalins, enkephalinase helps maintain the balance between pain relief and pain sensitivity.

In addition to pain modulation, enkephalinase is involved in various other physiological processes. It is known to regulate blood pressure by degrading vasoactive peptides such as bradykinin and substance P. Enkephalinase also plays a role in the regulation of mood and emotions, as enkephalins are involved in the reward system and the modulation of stress responses.

Clinical Significance

The activity of enkephalinase has been implicated in several medical conditions. Inhibitors of enkephalinase, such as thiorphan and racecadotril, have been used as therapeutic agents for the treatment of pain and hypertension. These inhibitors increase the levels of enkephalins, leading to prolonged analgesic effects and vasodilation.

Enkephalinase inhibitors have also shown potential in the treatment of mood disorders, such as depression and anxiety. By preventing the degradation of enkephalins, these inhibitors enhance the activity of the endogenous opioid system, which is involved in mood regulation.

See Also

• Opioid receptors
• Endogenous opioids
• Pain modulation
• Metalloprotease