SR142948A is a potent antagonist of the cardiovascular effects of neurotensin

Journal of Cardiovascular Pharmacology
P SchaefferJ M Herbert

Abstract

The novel compound SR142948A was compared with SR48692 as an antagonist of neurotensin-induced cardiovascular effects both in vitro and in vivo. SR142948A inhibited [125I]-neurotensin binding [median inhibitory concentration (IC50) = 0.24 +/- 0.01 nM], neurotensin-induced cytosolic free Ca2+ increase (IC50 = 19 +/- 6 nM), and prostacyclin production in human umbilical vein endothelial cells (IC50 = 17 +/- 3 nM) at much lower concentrations than did SR48692 (respective IC50 values, 14 +/- 5, 41 +/- 16, and 86 +/- 16 nM). Oral administration of SR142948A (10 microg/kg) resulted in significant inhibition of neurotensin-induced blood pressure changes, whereas SR48692 was active only at 10-fold higher doses. Furthermore, SR142948A administered i.v. in microg/kg quantities in the rat was as active as mg/kg doses of SR48692 on neurotensin-induced increase in hematocrit. SR142948A injected intradermally also significantly inhibited neurotensin-induced plasma extravasation at concentrations as low as 10 pmol/site, whereas 1,000 pmol/site of SR48692 were necessary to reach a significant inhibition. These data show that SR142948A is a novel, extremely potent antagonist of neurotensin-induced cardiovascular responses both in vitro and in v...Continue Reading

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Citations

Oct 18, 2000·Regulatory Peptides·B M Tyler-McMahonE Richelson
Jul 29, 2006·Peptides·Jean Mazella, Jean-Pierre Vincent
Jul 24, 2012·European Journal of Pharmacology·Katarzyna Kaczyńska, Małgorzata Szereda-Przestaszewska
May 26, 2015·European Journal of Pharmacology·Oleg E Osadchii
Apr 4, 2017·Journal of Medicinal Chemistry·Roberto FanelliFlorine Cavelier
Oct 17, 2019·International Journal of Molecular Sciences·Ewelina Russjan, Katarzyna Kaczyńska
May 26, 2009·ACS Chemical Biology·Rebecca M MyersSteven V Ley

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