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- W2009462810 abstract "We investigated the ability of the first non-peptide tachykinin NK3-receptor antagonist, SR142801, to antagonize contractions of guinea-pig intestinal tissues induced by the putative selective agonists [MePhe7]NKB and senktide. These agonists produced tetrodotoxin-sensitive responses presumably by acting on neuronal NK3-receptors. Indeed, tetrodotoxin (1 μM) fully prevented the [MePhe7]NKB and senktide elicited contractions in taenia caeci, ileum and its electrically stimulated myenteric plexus longitudinal muscle. SR142801 had no intrinsic agonist activity and dose-dependently antagonized the contractions elicited by [MePhe7]NKB or senktide. Its affinity for tachykinin NK3 receptors (mean apparent pKB, 8.98 ± 0.1 SEM) was not dependent on: the agonist, the different intestinal segments tested and the presence or absence of atropine. SR142801 appears to be a potent tachykinin receptor antagonist, selective for guinea-pig intestinal Nk3-receptors. Our findings also suggest that the cholinergic and non-cholinergic responses elicited by [MePhe7]NKB and senktide in the investigated tissues are mediated by the same neuronal tachykinin NK3 receptor." @default.
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- W2009462810 date "1995-10-01" @default.
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- W2009462810 title "Neuronal nk3-receptors in guinea-pig ileum and taenia caeci: in vitro characterization by their first non-peptide antagonist, sr142801" @default.
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- W2009462810 doi "https://doi.org/10.1016/0024-3205(95)02211-z" @default.
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