Bronchodilating properties of the VIP receptor agonist Ro 25-1553 compared to those of formoterol on the guinea-pig isolated trachea

Eur J Pharmacol. 2001 Nov 2;430(2-3):335-40. doi: 10.1016/s0014-2999(01)01299-7.


Ro 25-1553 is a 31-amino acid analogue of vasoactive intestinal peptide (VIP) and has recently been shown to be highly selective for the VPAC(2)-receptor. The bronchodilating property of this compound was evaluated in vitro on preparations of guinea-pig trachea, with the long-acting beta(2)-adrenoceptor selective agonist, formoterol, as a reference. In strip-preparations precontracted with carbachol, Ro 25-1553 caused a concentration-dependent and complete relaxation of the tracheal smooth muscle. Ro 25-1553 was 3-7 times less potent than formoterol on a molar basis, but the efficacy was comparable with that of formoterol. Both compounds showed a rapid onset of action and a similar durability of effect. Ro 25-1553 appeared to interact with formoterol as well as with salmeterol in an additive way. In vagus nerve-trachea tube preparations, when added to the external medium, Ro 25-1553 concentration-dependently and completely inhibited nerve-induced contractions. This occurred in the same concentration range as needed for relaxation of precontracted strips. Ro 25-1553 was active also when administered into the tracheal lumen albeit the concentration had to be increased. The present study supports and extends previous results suggesting that Ro 25-1553 may be a powerful alternative to the beta(2)-adrenoceptor agonists which prevail today.

Publication types

  • Comparative Study

MeSH terms

  • Albuterol / analogs & derivatives*
  • Albuterol / pharmacology
  • Amino Acid Sequence
  • Animals
  • Bronchodilator Agents / pharmacology*
  • Carbachol / pharmacology
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Electric Stimulation
  • Ethanolamines / pharmacology*
  • Formoterol Fumarate
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Molecular Sequence Data
  • Muscle Relaxation / drug effects
  • Peptides, Cyclic / pharmacology*
  • Receptors, Vasoactive Intestinal Peptide / agonists*
  • Salmeterol Xinafoate
  • Trachea / drug effects*
  • Trachea / innervation
  • Trachea / physiology
  • Vagus Nerve / physiology
  • Vasoactive Intestinal Peptide / analogs & derivatives*
  • Vasoactive Intestinal Peptide / pharmacology*


  • Bronchodilator Agents
  • Ethanolamines
  • Peptides, Cyclic
  • Receptors, Vasoactive Intestinal Peptide
  • Ro 25-1553
  • Vasoactive Intestinal Peptide
  • Salmeterol Xinafoate
  • Carbachol
  • Albuterol
  • Formoterol Fumarate