PMID: 7541694Apr 1, 1995Paper

Blockade of mast cell histamine secretion in response to neurotensin by SR 48692, a nonpeptide antagonist of the neurotensin brain receptor

British Journal of Pharmacology
L A MillerR S Feldberg

Abstract

1. Pretreatment of rat isolated mast cells with SR 48692, a nonpeptide antagonist of the neurotensin (NT) receptor, prevented histamine secretion in response to NT. 2. This inhibition was rapid in onset (approximately 1 min) and dependent upon the concentration of SR 48692 (IC50 approximately 1-10 nM). 3. SR 48692 (1-1000 nM) did not inhibit histamine secretion elicited by substance P, bradykinin or compound 48/80, or by anti-IgE stimulation of sensitized mast cells. 4. When SR 48692 was injected intradermally (5 pmol in 50 microliters) into anaesthetized rats, 15 min before the intradermal injection of NT, it reduced the effect of NT on vascular permeability. 5. When injected intravenously, SR 48692 attenuated the effects of NT on haematocrit and blood stasis. 6. These results demonstrate that SR 48692 selectively antagonizes the actions of NT on rat isolated mast cells as well as mast cells in vivo. Given the demonstrated specific interaction of SR 48692 with receptors for NT in brain, our results suggest the presence of specific NT receptors on mast cells.

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Citations

Mar 9, 2007·Inflammatory Bowel Diseases·Kara J Gross, Charalabos Pothoulakis
Sep 20, 2011·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·David E CochraneRoss S Feldberg
May 10, 2006·Proceedings of the National Academy of Sciences of the United States of America·Jill DonelanTheoharis C Theoharides
Feb 1, 1996·British Journal of Pharmacology·F MulèF Bonvissuto
Mar 17, 1999·The Journal of Clinical Investigation·I CastagliuoloC Pothoulakis
Feb 28, 2001·Expert Opinion on Investigational Drugs·T C Theoharides, G R Sant
May 10, 2011·Regulatory Peptides·Konstantinos Kalafatakis, Konstantinos Triantafyllou
Aug 26, 2010·British Journal of Pharmacology·E SickJ P Gies
Jun 27, 2003·Biochemical Pharmacology·David E CochraneHarry Bernheim
May 26, 2015·European Journal of Pharmacology·Oleg E Osadchii
Nov 3, 2016·Proceedings of the National Academy of Sciences of the United States of America·Arti B PatelTheoharis C Theoharides
Jul 18, 2014·Biology of Reproduction·Yuuki HiradateKentaro Tanemura
Dec 25, 2003·American Journal of Physiology. Gastrointestinal and Liver Physiology·Xianyong Gui, Robert E Carraway
Mar 15, 2005·American Journal of Physiology. Gastrointestinal and Liver Physiology·Paola BrunIgnazio Castagliuolo
Jan 22, 2019·The Journal of Reproduction and Development·Kohei UmezuKentaro Tanemura
Apr 29, 1998·Journal of Cardiovascular Pharmacology·P SchaefferJ M Herbert

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