Possible key residues that determine left gastric artery blood flow response to PACAP in dogs

World J Gastroenterol. 2010 Oct 14;16(38):4865-70. doi: 10.3748/wjg.v16.i38.4865.

Abstract

Aim: To determine the effect of pituitary adenylate cyclase-activating polypeptide (PACAP) on left gastric artery (LGA) flow and to unveil the structural or functional important sites that may be critical for discrimination of different receptor subtypes.

Methods: Peptides, including PACAP-27, PACAP-38, amino acid substituted PACAP-27 and C-terminus truncated analogues PACAP (27-38), were synthesized by a simultaneous multiple solid-phase peptide synthesizer. Flow probes of an ultrasound transit-time blood flowmeter were placed around the LGA of beagle dogs. When peptides were infused intravenously, the blood flow was measured.

Results: [Ala4, Val5]-PACAP-27 caused a concentration-dependent vasodepressor action which was similar to that caused by PACAP-27. The LGA blood flow response to [Ala4, Val5]-PACAP-27 was significantly higher than that to PACAP-27, which was similar to that to vasoactive intestinal polypeptide (VIP) at the same dose. [Ala6]-PACAP-27 did not increase the peak LGA flow. [Gly8]-PACAP-27 showed a similar activity to VIP. [Asn24, Ser25, Ile26]-PACAP-27 did not change the activity of peptides at all doses.

Conclusion: NH2 terminus is more important to biological activity of peptides and specific receptor recognition than COOH-terminus.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Arteries / drug effects*
  • Dogs
  • Hemodynamics / drug effects
  • Molecular Sequence Data
  • Peptides / chemical synthesis
  • Peptides / genetics
  • Peptides / pharmacology
  • Pituitary Adenylate Cyclase-Activating Polypeptide / genetics*
  • Pituitary Adenylate Cyclase-Activating Polypeptide / pharmacology*
  • Regional Blood Flow / drug effects*
  • Stomach / blood supply*
  • Vasoactive Intestinal Peptide / genetics
  • Vasoactive Intestinal Peptide / pharmacology

Substances

  • Peptides
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Vasoactive Intestinal Peptide