Abstract
Gourlet, P., A. Vandermeers, P. Vertongen, J. Rathe, P. De Neef, J. Cnudde, M. Waelbroeck and P. Robberecht. Development of high affinity selective VIP 1 receptor agonists. Peptides 18(10) 1539–1545, 1997.—The biological effects of VIP are mediated by at least two VIP receptors: the VIP 1 and the VIP 2 receptors that were cloned in rat, human and mice. As the mRNA coding for each receptor are located in different tissues, it is likely that each receptor modulates different functions. It is therefore of interest to obtain selective agonists for each receptor subtype. In the present work, we achieved the synthesis of two VIP 1 receptor selective agonists derived from secretin and GRF. [R 16]chicken secretin had IC 50 values of binding of 1, 10,000, 20, and 3000 nM for the rat VIP 1-, VIP 2-, secretin- and PACAP receptors, respectively. This peptide, however, had a weaker affinity for the human VIP 1 receptor (IC 50 of 60 nM). The chimeric, substituted peptide [K 15,R 16,L 27]VIP(1-7)/GRF(8-27) had IC 50 values of binding of 1, 10,000, 10,000 and 30,000 nM for the rat VIP 1-, VIP 2-, secretin- and PACAP receptors, respectively. Furthermore, its also showed an IC 50 of 0.8 nM for the human VIP 1 receptor and a low affinity for the human VIP 2 receptor. It is unlikely that this GRF analogue interacted with a high affinity to the pituitary GRF receptors as it did not stimulate rat pituitary adenylate cyclase activity. The two described analogues stimulated maximally the adenylate cyclase activity on membranes expressing each receptor subtype.
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