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 anti ...]
of
racecadotril. NEP-like enzymes include the
endothelin
Endothelins are peptides with 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 overexpressed, they contribute ...
-
converting enzymes.
The peptidase M13 family believed to activate or inactivate oligopeptide (pro)-hormones such as opioid peptides,
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 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 enkephalins by acting as an enkephalinase inhibitor
Inhibitor or inhibition may refer to:
In biology
* Enzyme inhib ...
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
*
Candoxatril
References
{{Opioidergics
Thioesters
Carboxylate esters
Drugs acting on the gastrointestinal system and metabolism