Further evidence that tachykinin-induced contraction of human isolated bronchus is mediated only by NK2-receptors

Neuropeptides
R L SheldrickR A Coleman

Abstract

The tachykinin-receptors mediating contraction of human bronchus have been characterized using both tachykinin-receptor selective agonists and blocking drugs under conditions where tachykinin metabolism by endogenous peptidases has been controlled, and true equilibrium conditions have been established. The findings that neurokinin A (EC50 = 2 nM) is the most potent agonist, and the NK2-receptor selective agonist, GR64349, is only 3-fold weaker, whereas agonists selective for NK1-receptors, substance P methyl ester, or NK3-receptors, senktide, are inactive, suggest that this effect is mediated exclusively by NK2-receptors. This is supported by observations that GR64349 is antagonised by the selective NK2-receptor blocking drugs, MEN10207 (pA2 = 6.7), R396 (pA2 = 6.1), (+/-)SR48968 (pA2 = 8.4) and GR159897 (pA2 = 8.6), but not by the NK1-receptor blocking drug, GR82334 (pA2 < 5). In approximately half of the preparations, the peptidase inhibitors, phosphoramidon (1 microM) and bestatin (100 microM), caused a marked and well-maintained contraction (approximately 20% of neurokinin A maximum), which may indicate a role for endogenous tachykinins in the regulation of tone in this preparation. This is supported by the finding that neu...Continue Reading

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Citations

Oct 18, 2000·European Journal of Pharmacology·A D KraneveldF P Nijkamp
Sep 11, 2002·European Journal of Pharmacology·John C AnthesRobert W Egan
Sep 12, 2002·European Journal of Pharmacology·Timothy J Martin, Kenneth J Broadley
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May 7, 1999·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·C AdvenierR Pauwels
Jan 22, 2008·American Journal of Physiology. Lung Cellular and Molecular Physiology·Kentaro MizutaCharles W Emala
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Nov 6, 2014·Biomolecular Concepts·Takenori Onaga
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