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• W2115166270 abstract "Tachykinin receptors in guinea-pig airways were examined using radioligand binding techniques in lung homogenates, and using isolated bronchial segments. Binding of the NK 1 selective radioligand 125 I-labelled Bolton–Hunter [Sar 9 ,Met(O 2 ) 11 ]substance P ([ 125 I]BHSarSP) was saturable and of high affinity (K D , 0.26 nM). The rank potency order of competitors for [ 125 I]BHSarSP binding was [Pro 9 ]SP > CP 96345 [Formula: see text] septide > [pGlu 6 ]SP(6–11) > RP 67580 ≥ [DPro 9 , [Formula: see text],Trp 11 ]SP > [DPro 9 ,[Formula: see text],Trp 11 ]physalaemin ≥ GR 82334 ≥ 127 I Bolton–Hunter neurokinin A (BHNKA). Septide had higher affinity than expected, and it was the only ligand to bind to two sites. Agonists interacting with NK 2 receptors were more potent contractile agents than NK 1 receptor agonists. Responses to BHNKA (pD 2 8.4) were antagonized by MDL 29913 and MEN 10207, with pK B values 6.42 and 6.79, and also by SR 48968 and GR 94800, although this was not dose dependent. This agonist was also weakly inhibited by CP 96345 and RP 67580. These data demonstrate that BHNKA can interact with both NK 1 and NK 2 receptors. There was no relationship between the binding affinity of NK 1 ligands in lung homogenates, with GR 82334 being notably weak, and their agonist or antagonist potency in bronchial smooth muscle.Key words: tachykinin receptor, radioligand binding, septide, guinea-pig bronchus, 127 I Bolton–Hunter neurokinin A." @default.
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• W2115166270 date "1995-07-01" @default.
• W2115166270 modified "2023-09-23" @default.
• W2115166270 title "Tachykinin receptors in guinea-pig airways: characterization using selective ligands" @default.
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• W2115166270 doi "https://doi.org/10.1139/y95-126" @default.
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