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首页> 外文期刊>Life sciences >In vitro characterization of the non-peptide tachykinin NK1 and NK2-receptor antagonists, SR140333 and SR48968 in different rat and guinea-pig intestinal segments.
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In vitro characterization of the non-peptide tachykinin NK1 and NK2-receptor antagonists, SR140333 and SR48968 in different rat and guinea-pig intestinal segments.

机译：在不同大鼠和豚鼠肠段中非肽速激肽NK1和NK2受体拮抗剂SR140333和SR48968的体外表征。

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摘要

We investigated the potent non-peptide tachykinin receptor antagonists SR140333 and SR48968 for their ability to prevent the contraction of isolated intestinal tissues elicited by the non-selective agonists substance P (SP) and neurokinin A (NKA), or by [Sar9,Met(O2)11]SP and [beta-Ala8]NKA-(4-10) that are selective agonists for NK1 and NK2 receptors, respectively. In guinea-pig ileum, containing mainly NK1-receptors: SR140333 caused a pseudo-irreversible blockade of contractions induced by either SP (KB, 0.01 nM) or [Sar9,Met(O2)11]SP (KB, 0.03 nM); SR140333 but not SR48968, dose-dependently (IC50, 0.06 nM) antagonized the contractions elicited by capsaicin. In rat duodenum, containing mainly NK2 receptors, SR48968 caused a parallel rightward shift of the concentration-response curves of [beta-Ala8]NKA-(4-10) (pA2, 9.5), but not of NKA. In rat esophageal tunica muscularis mucosae, SR48968 non-competitively antagonized [beta-Ala8]NKA-(4-10) and NKA. SR48968 and SR140333 thus appear to be potent tachykinin receptor antagonists, selective for intestinal receptors respectively of the NK2 and NK1 type. The results also suggest that rat esophagus might contain a NK2-receptor subtype different from that of rat duodenum.
机译：我们研究了有效的非肽速激肽受体拮抗剂SR140333和SR48968防止非选择性激动剂物质P（SP）和神经激肽A（NKA）或[Sar9，Met（ O2）11] SP和β-Ala8] NKA-（4-10）分别是NK1和NK2受体的选择性激动剂。在豚鼠回肠中，主要含有NK1受体：SR140333引起由SP（KB，0.01 nM）或[Sar9，Met（O2）11] SP（KB，0.03 nM）引起的收缩的假不可逆性阻断; SR140333而不是SR48968，剂量依赖性地（IC50，0.06 nM）拮抗辣椒素引起的收缩。在主要包含NK2受体的大鼠十二指肠中，SR48968引起β-Ala8] NKA-（4-10）（pA2，9.5）的浓度-响应曲线平行向右移动，但不引起NKA。在大鼠食管肌膜粘膜中，SR48968非竞争性拮抗[β-Ala8] NKA-（4-10）和NKA。因此，SR48968和SR140333似乎是有效的速激肽受体拮抗剂，对NK2和NK1型肠道受体具有选择性。结果还表明，大鼠食道可能含有不同于大鼠十二指肠的NK2受体亚型。

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