The long-acting vasoactive intestinal polypeptide agonist RO 25-1553 is highly selective of the VIP2 receptor subclass.

Abstract

RO 25-1553 is a synthetic VIP analogue that induced a long-lasting relaxation of tracheal and bronchial smooth muscles as well as a reduction of edema and eosinophilic mobilization during pulmonary anaphylaxis. In the present study, we tested in vitro the capacity of RO 25-1553 to occupy the different VIP/PACAP receptor subclasses and to stimulate adenylate cyclase activity. The cellular models tested expressed one single receptor subtype: Chinese hamster ovary (CHO) cells transfected with the rat recombinant PACAP I, rat VIP1, and human VIP2 receptors; SUP T1 cells expressing the human VIP2 and HCT 15 and LoVo cells expressing the human VIP1 receptor. RO 25-1553 was threefold more potent than VIP on the human VIP2 receptor, 100- and 600-fold less potent than VIP on the rat and human VIP1 receptors, respectively, and 10-fold less potent than VIP and 3000-fold less potent than PACAP on the PACAP I receptor. RO 25-1553 was a full agonist on the VIP2, the PACAP I, and the rat recombinant VIP1 receptor but a partial agonist only on the human VIP1 receptor. Thus, RO 25-1553 is a highly selective agonist ligand for the VIP2 receptor subclass.

• Authors: P Gourlet, P Vertongen, A Vandermeers, M C Vandermeers-Piret, J Rathe, P De Neef, M Waelbroeck, P Robberecht
• Journal: Peptides (Peptides) Vol. 18 Issue 3 Pg. 403-8 ( 1997) ISSN: 0196-9781 [Print] United States
• PMID: 9145428 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• ADCYAP1 protein, human
• Adcyap1 protein, rat
• Neuropeptides
• Peptides, Cyclic
• Pituitary Adenylate Cyclase-Activating Polypeptide
• Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
• Receptors, Pituitary Hormone
• Receptors, Vasoactive Intestinal Peptide
• Receptors, Vasoactive Intestinal Peptide, Type II
• Receptors, Vasoactive Intestinal Polypeptide, Type I
• Recombinant Proteins
• Ro 25-1553
• Vasoactive Intestinal Peptide
• Adenylyl Cyclases

Topics

• Adenylyl Cyclases (metabolism)
• Amino Acid Sequence
• Animals
• CHO Cells
• Cricetinae
• Enzyme Activation (drug effects)
• Humans
• Molecular Sequence Data
• Neuropeptides (chemical synthesis, pharmacology)
• Peptides, Cyclic (agonists, pharmacology)
• Pituitary Adenylate Cyclase-Activating Polypeptide
• Rats
• Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
• Receptors, Pituitary Hormone (drug effects)
• Receptors, Vasoactive Intestinal Peptide (chemistry, drug effects, metabolism)
• Receptors, Vasoactive Intestinal Peptide, Type II
• Receptors, Vasoactive Intestinal Polypeptide, Type I
• Recombinant Proteins
• Transfection
• Tumor Cells, Cultured
• Vasoactive Intestinal Peptide (agonists, analogs & derivatives, pharmacology)