Proteolysis of His-Phe-Arg-Trp-Pro-Gly-Pro in the blood and brain of rats in vivo

Dokl Biochem Biophys. 2015:464:301-4. doi: 10.1134/S1607672915050087. Epub 2015 Oct 31.

Abstract

The kinetics of the content of His-Phe-Arg-Trp-Pro-Gly-Pro (ACTH (6-9)PGP) and its hydrolysis products in the blood and brain of rats in the case of intranasal administration and intravenous injection of tritiated ACTH(6-9)PGP was studied. The parameters of bioavailability of ACTH(6-9)PGP administered intranasally were higher, indicating certain prospects in the intranasal application in clinical practice. We also found that the factor that determines ACTH(6-9)PGP proteolysis in experiments both in vivo and in vitro is aminopeptidases. The main products of ACTH(6-9)PGP during its metabolism in rats are short peptides and amino acids.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intranasal
  • Administration, Intravenous
  • Adrenocorticotropic Hormone / administration & dosage
  • Adrenocorticotropic Hormone / analogs & derivatives*
  • Adrenocorticotropic Hormone / pharmacokinetics
  • Animals
  • Brain / metabolism*
  • Central Nervous System Agents / administration & dosage
  • Central Nervous System Agents / metabolism*
  • Drug Stability
  • Kinetics
  • Peptide Fragments / administration & dosage
  • Peptide Fragments / blood
  • Peptide Fragments / metabolism
  • Peptide Fragments / pharmacokinetics*
  • Proteolysis
  • Rats
  • Time Factors

Substances

  • Central Nervous System Agents
  • His-Phe-Arg-Trp-Pro-Gly-Pro
  • Peptide Fragments
  • Adrenocorticotropic Hormone