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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References |
1. Fournié-Zaluski MC, Coric P, Turcaud S, Lucas E, Noble F, Maldonado R, Roques BP. (1992)
"Mixed inhibitor-prodrug" as a new approach toward systemically active inhibitors of enkephalin-degrading enzymes. J Med Chem, 35 (13): 2473-81. [PMID:1352352] |
2. Noble F, Soleilhac JM, Soroca-Lucas E, Turcaud S, Fournie-Zaluski MC, Roques BP. (1992)
Inhibition of the enkephalin-metabolizing enzymes by the first systemically active mixed inhibitor prodrug RB 101 induces potent analgesic responses in mice and rats. J Pharmacol Exp Ther, 261 (1): 181-90. [PMID:1560364] |