enkephalinase การใช้

• Various enkephalinase inhibitors, such as ketalorphan, spinorphin, and tynorphin, are mainly exopeptidase inhibitors.
• Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinase.
• As such, the analgesic effects of Na v 1.7 blockers may be greatly potentiated by the co-administration of exogenous opioids or enkephalinase inhibitors.
• "' Racecadotril "', also known as "'acetorphan "', is an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor.
• 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.
• Unlike the more commonly used enkephalinase inhibitor racecadotril, which only acts peripherally and has antidiarrheal effects, RB-101 is able to enter the brain, and thus produces a range of effects, acting as an analgesic, anxiolytic and antidepressant.
• These antidepressant effects have been linked to endogenous opioid peptides acting at ? and ? opioid receptors, and so can also be produced by enkephalinase inhibitors such as RB-101 . ] However, in human models the data for antidepressant effects remains inconclusive.
• The peptidase M13 family believed to activate or inactivate oligopeptide ( pro )-hormones such as opioid peptides, Thermolysin complexed with the inhibitor ( " S " )-thiorphan are isomeric thiol-containing inhibitors of endopeptidase EC 24-11 ( also called " enkephalinase " ).
• Immune regulating proteins found in prostasomes include : amino-peptidase N ( CD13 ); dipeptidyl-peptidase IV ( CD26 ); enkephalinase ( neutral endopeptidase, CD10 ); angiotensin converting enzyme ( ACE, CD143 ); tissue factor TF ( CD142, thromboplastin ); decay accelerating factor ( CD55 ); protectin ( CD59, inhibitor of MAC ) and complement regulatory membrane cofactor protein ( CD46 ).