Antihypertensive activity during inhibition of neutral endopeptidase and angiotensin converting enzyme

J Cardiovasc Pharmacol. 1991 Mar;17(3):456-65. doi: 10.1097/00005344-199103000-00015.

Abstract

The specific neutral endopeptidase (NEP) inhibitor, SQ 29,072 (7-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]amino]heptanoic acid), was studied in conscious spontaneously hypertensive rats (SHRs) and in DOCA/salt hypertensive rats during inhibition of angiotensin-converting enzyme (ACE) activity with captopril or SQ 27,519 (the free acid of fosinopril). In the SHR, the maximal depressor responses to the combination of SQ 29,072 and SQ 27,519 (-44 +/- 4 mm Hg) were greater than the responses to any of the inhibitors given alone (-26 +/- 5, -40 +/- 10, and -28 +/- 6 mm Hg for SQ 29,072, captopril, and SQ 27,519, respectively). In contrast, the maximal antihypertensive activities of SQ 29,072 were the same in conscious DOCA/salt hypertensive rats infused with saline, captopril, or SQ 27,519 (-54 +/- 10, -51 +/- 8, and -58 +/- 11 mm Hg, respectively), indicating a lack of synergism in this model. In agreement, SQ 28,133 [N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-L-leucine], a compound that inhibits both NEP and ACE, elicited significant depressor activities in both SHR and DOCA/salt hypertensive rats. In conclusion, a selective NEP inhibitor enhanced the depressor activity of ACE inhibitors in the conscious SHR, indicating that these agents may be effectively combined for treatment of some types of hypertension.

MeSH terms

  • Amino Acids / pharmacology*
  • Angiotensin-Converting Enzyme Inhibitors / pharmacology*
  • Animals
  • Antihypertensive Agents / pharmacology*
  • Blood Pressure / drug effects
  • Captopril / pharmacology
  • Fosinopril* / analogs & derivatives*
  • Hypertension / physiopathology
  • Male
  • Neprilysin / antagonists & inhibitors*
  • Organophosphorus Compounds / pharmacology
  • Proline / analogs & derivatives
  • Proline / pharmacology
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred Strains
  • Sulfhydryl Compounds / pharmacology*

Substances

  • Amino Acids
  • Angiotensin-Converting Enzyme Inhibitors
  • Antihypertensive Agents
  • Organophosphorus Compounds
  • Sulfhydryl Compounds
  • SQ 29072
  • Proline
  • Captopril
  • Neprilysin
  • Fosinopril
  • fosinoprilat