PMID: 9437716Jan 1, 1997Paper

In vitro properties of a high affinity selective antagonist of the VIP1 receptor

Peptides
P GourletP Robberecht

Abstract

A selective high affinity VIP1 receptor antagonist [Acetyl-His1, D-Phe2, Lys15, Arg16, Leu17] VIP(3-7)/GRF(8-27) or PG 97-269 was synthesized, by analogy with recently obtained selective VIP1 receptor agonists. The properties of the new peptide were evaluated on Chinese hamster ovary (CHO) cell membranes expressing either the rat VIP1-, rat VIP2- or the human VIP2-recombinant receptors and on LoVo cell membranes expressing exclusively the human VIP1 receptor. The IC50 values of 125I-VIP binding inhibition by PG 97-269 were 10, 2000, 2 and 3000 nM on the rat VIP1-, rat VIP2-, human VIP1- and human VIP2 receptors, respectively. PG 97-269 had a negligible affinity for the PACAP I receptor type. It did not stimulate adenylate cyclase activity, but inhibited competitively effect of VIP on the VIP1 receptor mediated stimulation of adenylate cyclase activity. The Ki values were respectively of 15 +/- 5 nM and 2 +/- 1 nM for the rat and human VIP1 receptors. Thus the described molecule in the first reported VIP antagonist with an affinity in the nM range and with a high selectivity for the VIP1 receptor subclass. It may be useful for evaluation of the physiological role of VIP in rat and human tissues.

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Citations

Jan 4, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Satomi OnoueShizuo Yamada
Jul 2, 2008·Journal of Molecular Neuroscience : MN·Alain CouvineauMarc Laburthe
Nov 14, 2013·Neuropeptides·Sanbing ShenDavid A Collier
Sep 3, 1998·European Journal of Pharmacology·P GourletP Robberecht
Nov 27, 1998·European Journal of Pharmacology·P RobberechtR A Lefebvre
Nov 26, 2002·Journal of Neuroimmunology·Xiuju JiangDoina Ganea
Aug 4, 1999·Trends in Pharmacological Sciences·T Dickinson, S M Fleetwood-Walker
Sep 11, 2002·Regulatory Peptides·M Laburthe, A Couvineau
Feb 11, 2003·Peptides·Terry W MoodyRobert T Jensen
May 22, 2002·Cellular Signalling·Ingrid LangerMagali Waelbroeck
May 24, 2003·Trends in Molecular Medicine·David Pozo
Aug 28, 1998·British Journal of Pharmacology·B Y De WinterP A Pelckmans
Oct 13, 2000·British Journal of Pharmacology·G E BoeckxstaensP J Blommaart
Aug 30, 2000·Proceedings of the National Academy of Sciences of the United States of America·G HalmosT Czompoly
Feb 3, 1999·Annals of the New York Academy of Sciences·P Robberecht, M Waelbroeck
Apr 17, 2010·Journal of Applied Physiology·Dean L KelloggJohn M Johnson
Oct 12, 2012·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Jun-Hyeong ChoVadim Y Bolshakov
May 9, 2014·Journal of Molecular Neuroscience : MN·Rebeca JimenoYasmina Juarranz
Oct 28, 2003·The Journal of Physiology·Lionel FizanneBérengère Fromy
May 18, 2010·Respiratory Physiology & Neurobiology·Melissa M J Farnham, Paul M Pilowsky
Feb 19, 2009·European Journal of Pharmacology·Qingqiong LuoLingyun Xu
Dec 27, 2008·Pharmacology & Therapeutics·Louise Dickson, Keith Finlayson

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