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. 1995 Apr;273(1):161-7.

Superactive lipophilic peptides discriminate multiple vasoactive intestinal peptide receptors

I Gozes  1 , G Lilling, R Glazer, A Ticher, I E Ashkenazi, A Davidson, S Rubinraut, M Fridkin, D E Brenneman
Affiliations
  • PMID: 7714762

Superactive lipophilic peptides discriminate multiple vasoactive intestinal peptide receptors

I Gozes et al. J Pharmacol Exp Ther. 1995 Apr.

Abstract

To distinguish vasoactive intestinal peptide (VIP) receptors in the brain-mediating neurotransmission and neurotrophism, potent VIP analogues were designed. Using a single amino acid substitution and the addition of a fatty acyl moiety, an analogue was devised that exhibited both a 100-fold greater potency than VIP and specificity for a VIP receptor associated with neuronal survival. This VIP agonist increased neuronal survival via a cAMP-independent mechanism. Identical chemical modification of a prototype VIP antagonist (Met-Hybrid, Neurotensin6-11-VIP7-28) also resulted in a 100-fold greater potency in blocking VIP-mediated increases in neuronal survival. Blockade of circadian activity rhythms was limited to VIP antagonists that could inhibit VIP-mediated increases in cAMP. These lipophilic peptides provide novel tools in receptor discrimination and drug design.

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