Activity-dependent neurotrophic factor: intranasal administration of femtomolar-acting peptides improve performance in a water maze

J Pharmacol Exp Ther. 2000 Jun;293(3):1091-8.

Abstract

Activity-dependent neurotrophic factor (ADNF) is a glia-derived protein that is neuroprotective at femtomolar concentrations. A nine-amino acid peptide derived from ADNF (Ser-Ala-Leu-Leu-Arg-Ser-Ile-Pro-Ala; ADNF-9) captured the activity of the parent protein and has been reported to protect cultured neurons from multiple neurotoxins. Antibodies recognizing ADNF-9 produced neuronal apoptosis, and identified an additional, structurally related, glia-derived peptide, Asn-Ala-Pro-Val-Ser-Ile-Pro-Gln (NAP). Previous comparative studies have characterized s.c.-injected NAP as most efficacious in protecting against developmental retardation and learning impairments in apolipoprotein E-deficient mice. This study was designed to assess 1) neuroprotection after intranasal administration of ADNF-9 and NAP to rats treated with the cholinotoxin ethylcholine aziridium; and 2) bioavailability and pharmacokinetics after intranasal administration. Results showed significant improvements in short-term spatial memory, as assessed in a water maze, after daily intranasal administration of 1 microg of peptide (ADNF-9 or NAP) per animal. However, a 5-day pretreatment with ADNF-9 did not improve performance measured after cessation of treatment. Compared with rats treated with ADNF-9, NAP-pretreated animals exhibited a significantly better performance. Furthermore, NAP (and not ADNF-9) protected against loss of choline acetyl transferase activity. Significant amounts of (3)H-labeled NAP reached the brain, remained intact 30 min after administration, and dissipated 60 min after administration. This study revealed efficacy for ADNF-related peptides in rodent models for neurodegeneration. The small size of the molecules, the low dosage required, the noninvasive administration route, and the demonstrated activity in a relevant paradigm suggest NAP as a lead compound for future drug design.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Administration, Intranasal
  • Animals
  • Aziridines / pharmacology
  • Biological Availability
  • Choline / analogs & derivatives
  • Choline / pharmacology
  • Choline O-Acetyltransferase / metabolism
  • Drug Stability
  • Male
  • Maze Learning / drug effects*
  • Memory Disorders / prevention & control
  • Nerve Growth Factor / pharmacology*
  • Nerve Tissue Proteins / administration & dosage
  • Nerve Tissue Proteins / pharmacokinetics
  • Nerve Tissue Proteins / pharmacology*
  • Neuroprotective Agents / pharmacology*
  • Rats
  • Rats, Wistar

Substances

  • Aziridines
  • Nerve Tissue Proteins
  • Neuroprotective Agents
  • Nerve Growth Factor
  • ethylcholine aziridinium
  • Choline O-Acetyltransferase
  • Choline