PMID: 7512696Jan 1, 1994Paper

Evidence for tachykinin NK-2 receptors in guinea-pig airways from binding and functional studies, using [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10)

Neuropeptides
X P ZengE Burcher

Abstract

The potent contractile responses of guinea-pig airways to neurokinin A (NKA) and neuropeptide gamma (NP gamma) are thought to be mediated by NK-2 receptors. However, NK-2 binding sites are not detectable using the radioligand [125I]-iodohistidyl-NKA. Here, a novel, highly selective iodinated radioligand, [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), and a number of related peptides have been used to characterize NK-2 receptors on guinea-pig airways, using binding and functional studies. Specific binding of [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), was saturable and to a single high affinity site, with KD 1.29 +/- 0.36 nM (n = 4). The rank order of potency for tachykinins and analogues as competitors for the binding was: [Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10) > or = NP gamma > or = [Lys5,MeLeu9,Nle10]-NKA(4-10) > NKA > or = SR 48968 > MDL 29913 > or = substance P (SP) = [127I]-Bolton-Hunter NKA (BHNKA) > or = MEN 10207 > neurokinin B (NKB). Septide, [DPro9,Pro10,Trp11]-SP, the NK-1 selective ligands [Sar9,Met(O2)11]-SP, [Pro9]-SP and CP 96345, the NK-3 selective senktide, and calcitonin gene-related peptide (CGRP) were weak or ineffective. On guinea-pig isolated bronchi, the potency order of contractile agonists was: [Lys5...Continue Reading

References

Sep 1, 1991·British Journal of Pharmacology·R PatacchiniC A Maggi
May 31, 1991·Biochemical and Biophysical Research Communications·A GrahamI Briggs
Nov 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·R LauferZ Selinger
Jan 1, 1989·Pulmonary Pharmacology·E BurcherN M O'Flynn

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Citations

May 23, 1998·European Journal of Pharmacology·A M ReynoldsR Scicchitano
Aug 26, 1998·European Journal of Pharmacology·M A MatuszekE Burcher
Apr 27, 2000·Allergy·G F JoosR A Pauwels
Mar 1, 1996·The Journal of Urology·X P Zeng, E Burcher
May 1, 1995·The Journal of Urology·X P ZengE Burcher
May 15, 2001·American Journal of Physiology. Lung Cellular and Molecular Physiology·K J HaleyC M Lilly

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