N-terminal galanin fragments inhibit the hippocampal release of acetylcholine in vivo

Brain Res. 1993 May 28;612(1-2):258-62. doi: 10.1016/0006-8993(93)91670-n.

Abstract

Using synthetic N-terminal fragments of galanin, galanin (1-7), galanin (1-9), galanin (1-12) and galanin (1-16), we have shown that the minimal sequence required for inhibition of acetylcholine release in vivo from rat ventral hippocampus corresponds to galanin (1-12). The fragment (1-9) displays activity in vivo but only at a very high concentration of 6.23 nmol while galanin (1-7) and C-terminal fragment (17-29) are without effect. Binding studies showed that galanin (1-16) and galanin (1-12) bind with submicromolar IC50 values to rat hippocampal galanin receptors. Galanin (1-9) has substantially lower affinity towards rat ventral hippocampal galanin receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / metabolism*
  • Animals
  • Binding, Competitive / drug effects
  • Galanin
  • Hippocampus / drug effects
  • Hippocampus / metabolism*
  • In Vitro Techniques
  • Ligands
  • Male
  • Membranes / drug effects
  • Membranes / metabolism
  • Neuropeptides / pharmacology*
  • Peptide Fragments / pharmacology*
  • Peptides / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Rats, Sprague-Dawley
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone / drug effects
  • Receptors, Gastrointestinal Hormone / metabolism
  • Scopolamine / antagonists & inhibitors
  • Scopolamine / pharmacology
  • Structure-Activity Relationship

Substances

  • Ligands
  • Neuropeptides
  • Peptide Fragments
  • Peptides
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone
  • Galanin
  • Scopolamine
  • Acetylcholine