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

par Gourlet, Philippe ;Vertongen, Pascale ;Vandermeers, André ;Vandermeers-Piret, Marie-Claire ;Rathe, Jean ;De Neef, Philippe ;Waelbroeck, Magali ;Robberecht, Patrick
Référence Peptides, 18, 3, page (403-408)
Publication Publié, 1997

Article révisé par les pairs

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Résumé :

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 1, rat VIP1, and human VIP2 receptors; SUPT1 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 1 receptor. RO 25-1553 was a full agonist on the VIP2, the PACAP 1, 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.