Regulation of H1-receptor coupling and H1-receptor mRNA by histamine in bovine tracheal smooth muscle

British Journal of Pharmacology
J L PypeG M Verleden

Abstract

1. Pretreatment of bovine tracheal smooth muscle (BTSM) with histamine (1-100 microM, 1 h) induced a concentration-dependent desensitization of the contractile response to subsequently administered histamine, with a reduction of the maximum response of 72 +/- 8% (n = 5) following pre-exposure to 100 microM histamine. In contrast, concentration-response curves to the muscarinic agonist, methacholine were not affected following histamine pretreatment, indicating a homologous desensitization. Furthermore, concentration-response curves to NaF, a G-protein activator, were not altered following histamine pre-incubation. 2. The histamine H1-receptor (H1R) desensitization could be antagonized by mepyramine (an H1-receptor antagonist, 1 microM) but not by cimetidine (an H2-receptor antagonist, 10 microM), indicating that the desensitization occurred via stimulation of histamine H1-receptors, without evidence for the involvement of histamine H2-receptors. 3. Indomethacin (10 microM) did not block the H1R desensitization, suggesting no involvement of prostaglandins. Furthermore, histamine pre-incubation in calcium free medium still induced a functional uncoupling of H1R. 4. GF 109203X, a protein kinase C (PKC) inhibitor, and H-7, a non-se...Continue Reading

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Citations

Nov 1, 1988·Trends in Pharmacological Sciences·P J BarnesJ Maclagan
Nov 17, 1998·American Journal of Respiratory and Critical Care Medicine·P J Barnes
Apr 3, 2001·American Journal of Respiratory and Critical Care Medicine·J L PypeG M Verleden
Oct 30, 2007·The Journal of Clinical Investigation·Rajkumar NoubadeCory Teuscher
Aug 9, 2005·British Journal of Pharmacology·Timothy J SelfStephen J Hill
Oct 18, 2001·Pulmonary Pharmacology & Therapeutics·P J Barnes

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