Mixed-inhibitor-prodrug as a new approach toward systemically active inhibitors of enkephalin-degrading enzymes

MC Fournie-Zaluski, P Coric, S Turcaud…

Index: Fournie-Zaluski, Marie-Claude; Coric, Pascal; Turcaud, Serge; Lucas, Evelyne; Noble, Florence; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 13 p. 2473 - 2481

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Citation Number: 158

Abstract

RB 101 [HzNCH (CHzCH~ CH~ CH~ SCHzCH (CHzPh) CONHCH (CH~ Ph) COOCHzPh] after iv administration were three times greater than those of a similar combined dose of its two constitutive moieties. The separation of the two diastereoisomers constituting RB 101 showed that the analgesia has a stereochemical dependence, the (S, S, S)-isomer being more active than the (SJZ, S)-isomer. Furthermore, in the tail flick test in the rat, RB 101 ...