Synonyms: RB 101 | RB-101
Compound class:
Synthetic organic
Comment: RB101 is an enkephalinase inhibitor, that is used as a biological tool [2]. It is metabolically cleaved into two active components, each of which inhibits one of the zinc-metallopeptidase enkephalin-degrading enzymes, aminopeptidase N (APN; ANPEP) and neutral endopeptidase (neprilysin; official gene name membrane metalloendopeptidase MME) [1]. Aminopeptidase N/neprilysin inhibition with RB101 induces an elevation in the levels of the two endogenous enkephalins [Met]enkephalin and [Leu]enkephalin. Prodrugs with this mechanism of action are known collectively as Dual Enkephalinase Inhibitors, or DENKIs.
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Bioactivity Comments |
The active components of RB101 are (S)2-amino-1-mercapto-4-methylthio butane (inhibits aminopeptidase N, IC50 11 nM) and N-[(R,S)-2-mercapto-methyl-1-oxo-3-phenylpropyl]-L-phenylalanine (inhibits neutral endopeptidase, IC50 2 nM) [2]. |