Enkephalinase inhibitor
Encyclopedia
An enkephalinase inhibitor is a type of enzyme inhibitor
Enzyme inhibitor
An enzyme inhibitor is a molecule that binds to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used as herbicides and pesticides...

 which inhibits one or more members of the enkephalinase
Enkephalinase
Enkephalinases are enzymes which degrade endogenous enkephalin opioid peptides. They include:* Aminopeptidase N * Neutral endopeptidase * Dipeptidyl peptidase 3 * Carboxypeptidase A6 * Angiotensin-converting enzyme...

 class of enzyme
Enzyme
Enzymes are proteins that catalyze chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical reactions in a biological cell need enzymes in order to occur at rates...

s that break down the endogenous
Endogenous
Endogenous substances are those that originate from within an organism, tissue, or cell. Endogenous retroviruses are caused by ancient infections of germ cells in humans, mammals and other vertebrates...

 enkephalin
Enkephalin
An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, or specifically endorphins, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin were revealed, one...

 opioid peptide
Opioid peptide
Opioid peptides are short sequences of amino acids that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides. Opioid peptides may be produced by the body itself, for example endorphins. The effects of these peptides vary, but they all resemble opiates...

s.

Some examples of enkephalinase inhibitors include bestatin, BL-2401, kelatorphan
Kelatorphan
Kelatorphan is a drug which acts as a powerful and complete inhibitor of nearly all of the enzymes responsible for catabolism of the endogenous enkephalins, including neutral endopeptidase , dipeptidyl peptidase III , aminopeptidase N , and angiotensin-converting enzyme...

, D-phenylalanine, racecadotril
Racecadotril
Racecadotril, also known as acetorphan, is an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor. Unlike other medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect—it reduces the secretion of water and...

, RB-101
RB-101
RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research.RB-101 is a prodrug which acts by splitting at the disulfide bond once inside the brain, to form two selective enzyme inhibitors and blocking both types of the zinc-metallopeptidase enkephalinase enzymes....

, RB-120, RB-3007, thiorphan
Thiorphan
Thiorphan is the active metabolite of the antidiarrheal racecadotril . It prevents the degradation of endogenous enkephalins by acting as an enkephalinase inhibitor....

, tynorphin
Tynorphin
Tynorphin is a synthetic opioid peptide which is a potent and competitive inhibitor of the enkephalinase class of enzymes which break down the endogenous enkephalin peptides...

, and ubenimex
Ubenimex
Ubenimex , also known as bestatin, is a competitive protease inhibitor. It is an inhibitor of aminopeptidase B, leukotriene A4 hydrolase , aminopeptidase N. It is being studied for use in the treatment of acute myelocytic leukemia....

, as well as the endogenous compounds opiorphin
Opiorphin
Opiorphin is an endogenous chemical compound first isolated from human saliva. Initial research with mice shows the compound has a painkilling effect greater than that of morphine. It works by stopping the normal breakdown of enkephalins, natural pain-killing opioids in the spinal cord...

 and spinorphin
Spinorphin
Spinorphin is an endogenous, non-classical opioid peptide of the hemorphin family, which was first isolated from the bovine spinal cord and acts as a regulator of the enkephalinases, a class of enzymes which break down endogenous the enkephalin peptides...

.

Analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....

, anticraving, antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...

, anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

, and antidiarrheal effects are common properties of enkephalinase inhibitors.
The source of this article is wikipedia, the free encyclopedia.  The text of this article is licensed under the GFDL.
 
x
OK