NK2 tachykinin receptors and contraction of circular muscle of the human colon: characterization of the NK2 receptor subtype.
作者： Sandro Giuliani , Gabriele Barbanti , Damiano Turini , Laura Quartara , Paolo Rovero
DOI: 10.1016/0014-2999(91)90892-T
关键词: Tachykinin receptor 、 Thiorphan 、 Receptor 、 Neurokinin A 、 Substance P 、 Internal medicine 、 Agonist 、 Biology 、 Peptide hormone 、 Endocrinology 、 Carbachol
摘要: Abstract The contractile effect of substance P, neurokinin A, receptor selective agonists for tachykinin receptors and NK 2 antagonists was investigated in mucosa-free circular strips the human isolated colon. Neurokinin A P produced concentration-dependent contractions which approached 80–90% maximal response to carbachol. about 370 times more potent than P. action not modified by peptidase inhibitors (bestatin, captopril thiorphan, 1 μM each). agonist, [β3-Ala 8 ]neurokinin A-(4–10) closely mimicked while 3 were active only at concentrations. pseudopeptide, MDL 28,564, is one most ligands available, behaved as a full agonist. Responses [β-Ala antagonized antagonists, with rank order potency MEN 10,376 > L 659,877 R 396. These data indicate that play dominant role determining contraction muscle colon peptides this family. subtype responsible belongs same (NK 2A ) previously identified rabbit pulmonary artery guinea-pig bronchi.
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