TABLE 2

Relative neutral endopeptidase (NEP) inhibition in tissues after single dose oral treatments of normal rats

Race 1 hCandox 1 hSac 1 hUK 1 hRace 5 hCandox 5 hSac 5 hUK 5 h
Kidney56%99%100%99%39%45%90%86%
Lung75%98%99%99%59%52%79%94%
Duodenum98%100%100%100%85%97%99%99%
Jejunum90%100%99%100%32%92%97%98%
  • NEP inhibitors were administered to normal healthy rats by oral gavage at the following doses: racecadotril (Race) 100 mg/kg, candoxatril (Candox) 150 mg/kg, sacubitril (Sac) 100 mg/kg, and UK-505,749 (UK) 100 mg/kg. Tissue lysates were prepared after 1 and 5 h, and NEP activity was measured as described in Materials and Methods. Percentage inhibition is the relative reduction in activity compared with vehicle-treated control animals.