Ecadotril is a
neutral endopeptidase
Neprilysin (), also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10), and common acute lymphoblastic leukemia antigen (CALLA) is an enzyme that in humans is encoded by the ''MME'' ge ...
inhibitor ((NEP
) EC 3.4.24.11
) and determined by the presence of peptidase family M13 as a neutral endopeptidase inhibited by
phosphoramidon
Phosphoramidon is a chemical compound derived from cultures of '' Streptomyces tanashiensis''. It is an inhibitor of the enzyme thermolysin, of the membrane metallo-endopeptidase,[enantiomer
In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''; from Ancient Greek ἐνάντιος ''(enántios)'' 'opposite', and μέρος ''(méros)'' 'part') – also called optical isomer, antipode, or optical ant ...]
of
racecadotril
Racecadotril, also known as acetorphan, is an antidiarrheal medication which acts as a peripheral enkephalinase inhibitor. Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretor ...
. NEP-like enzymes include the
endothelin
Endothelins are peptides with receptor (biochemistry), receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood pressure. The endothelins are normally kept in balance by other mechanisms, but when gene ex ...
-
converting enzymes.
The peptidase M13 family believed to activate or inactivate oligopeptide (pro)-hormones such as opioid peptides,
neprilysin
Neprilysin (), also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10), and common acute lymphoblastic leukemia antigen (CALLA) is an enzyme that in humans is encoded by the ''MME'' ge ...
is another member of this group, in the case of the metallopeptidases and aspartic, the nucleophiles clan or family for example MA, is an activated water molecule.
The peptidase domain for members of this family also contains a bacterial member and resembles that of
thermolysin
Thermolysin (, ''Bacillus thermoproteolyticus neutral proteinase'', ''thermoase'', ''thermoase Y10'', ''TLN'') is a thermostable neutral metalloproteinase enzyme produced by the Gram-positive bacteria ''Bacillus thermoproteolyticus''. It requires ...
the predicted active site residues for members of this family and thermolysin occur in the motif HEXXH.
Thermolysin complexed with the inhibitor (''S'')-
thiorphan
Thiorphan is the active metabolite of the antidiarrheal racecadotril (acetorphan). It prevents the degradation of endogenous enkephalin
An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are t ...
are isomeric thiol-containing inhibitors of endopeptidase EC 24-11
(also called "
enkephalinase Enkephalinases are enzymes that degrade endogenous enkephalin opioid peptides. They include:
* Aminopeptidase N (APN)
* Neutral endopeptidase (NEP)
* Dipeptidyl peptidase 3 (DPP3)
* Carboxypeptidase A6 (CPA6)
* Leucyl/cystinyl aminopeptidase ( ...
").
See also
*
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 ty ...
*
Candoxatril
Candoxatril is the orally active prodrug of candoxatrilat (UK-73967).
Human neutral endopeptidase
Human neutral endopeptidase ( neprilysin) as the neutral endopeptidase 24.11 complexed (RB-101) with phosphoramidon degrades and inactivates a numb ...
References
{{Opioidergics
Thioesters
Carboxylate esters
Drugs acting on the gastrointestinal system and metabolism