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- W2010010086 abstract "1 We studied the effect of the natural tachykinins and of synthetic agonists selective for the tachykinin NK1, NK2 and NK3 receptors, on the motility of guinea-pig isolated common bile duct longitudinally-oriented smooth muscle. 2 All the tachykinins tested (both natural and synthetic) produced a concentration-dependent contractile response of the guinea-pig isolated common bile duct: these effects underwent a marked tachyphylaxis, especially the responses elicited by NK1 and NK3 receptor-selective agonists. 3 Among the natural tachykinins neurokinin B (EC50=3.2 nm; 95% c.l.=2.0–5.1; n=4) was the most potent, being about 40 and 25 fold more potent than substance P (EC50=121.6 nm; 95% c.l.=94–157; P<0.01; n=4) and neurokinin A (EC50=83.4 nm; 95% c.l.=62–112; P<0.01; n=4), respectively. Among the synthetic analogues the NK3 receptor-selective agonist senktide (EC50=1.1 nm; 95% c.l.=0.7–1.8; n=8) was the most potent, being about 120, 110 and 20 fold more potent than [Sar9]substance P sulfone (NK1 receptor-selective) (EC50=130.4 nm; 95% c.l.=99–172; P<0.01; n=8), [βAla8]NKA (4–10) (NK2 receptor-selective) (EC50=120.1 nm; 95% c.l.=95–151; P<0.01; n=8) and septide (NK1 receptor-selective) (EC50=22.6 nm; 95% c.l.=18–28; P<0.01; n=8), respectively. All tachykinins (natural or synthetic receptor agonists) produced a similar Emax, averaging about 50% of that produced by KCl (80 mm). 4 Atropine (1 μm) did not affect the responses to either NK1 or NK2 receptor-selective agonists, whereas it reduced the Emax of senktide by about 50%, without affecting its potency (EC50). Tetrodotoxin (1 μm) totally blocked senktide-induced contractions, as did the combined pretreatment with atropine plus the tachykinin NK1 and NK2 receptor-selective antagonists GR 82334 and MEN 11420 (1 μm each), respectively. 5 GR 82334 (1 μm) blocked with apparent competitive kinetics septide- (apparent pKB=7.46±0.10; n=5) and [Sar9]substance P sulfone- (apparent pKB=6.80±0.04; n=4) induced contractions. MEN 11420 (30–300 nm), a novel potent NK2 receptor antagonist, potently antagonized [βAla8]NKA (4–10), with competitive kinetics (pKB=8.25±0.08; n=12: Schild plot slope=−0.90; 95% c.l.=−1.4; −0.35). The NK3 receptor-selective antagonist SR 142801 (30 nm) produced insurmountable antagonism of the senktide-induced contractions (Emax inhibited by 64%). None of the above antagonists, tested at the highest concentrations employed against tachykinins, affected the concentration–response curve to methacholine (0.1–300 μm). 6 We conclude that tachykinins produce contraction of the guinea-pig isolated common bile duct by stimulating NK1, NK2 and NK3 receptors. The responses obtained by activating NK1 and NK2 receptors are atropine-resistant. The contraction obtained by stimulating NK3 receptors is totally neurogenic, being mediated by the release of endogenous acetylcholine and tachykinins; the latter act, in turn, on postjunctional tachykinin NK1/NK2 receptors. The role of the NK3 receptor as prejunctional mediator of the excitatory transmission operated by tachykinins is discussed." @default.
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- W2010010086 date "1997-12-01" @default.
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- W2010010086 title "Characterization of receptors mediating contraction induced by tachykinins in the guinea-pig isolated common bile duct" @default.
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- W2010010086 doi "https://doi.org/10.1038/sj.bjp.0701560" @default.
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