The Long-Acting Vasoactive Intestinal Polypeptide Agonist RO 25-1553 Is Highly Selective of the VIP 2 Receptor Subclass

Jan 1, 1997Peptides

The long-lasting VIP-like drug RO 25-1553 targets the VIP2 receptor subtype

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Abstract

RO 25-1553 is threefold more potent than VIP on the human VIP2 receptor.

RO 25-1553 induced relaxation of tracheal and bronchial smooth muscles.
It reduced edema and eosinophilic mobilization during pulmonary anaphylaxis.
The compound acted as a full agonist on the VIP2, PACAP I, and rat VIP1 receptors.
It was a partial agonist on the human VIP1 receptor.
RO 25-1553 displayed varying potency across different receptor subclasses.

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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.

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The Long-Acting Vasoactive Intestinal Polypeptide Agonist RO 25-1553 Is Highly Selective of the VIP 2 Receptor Subclass

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