缓激肽（BK）1受体拮抗剂可阻断辣椒素诱导的小鼠耳部炎症。
A bradykinin (BK)1 receptor antagonist blocks capsaicin-induced ear inflammation in mice.
作者信息
Mantione C R, Rodriguez R
机构信息
Nova Pharmaceutical Corporation, Baltimore, Maryland 21224-2788.
出版信息
Br J Pharmacol. 1990 Mar;99(3):516-8. doi: 10.1111/j.1476-5381.1990.tb12960.x.
Abstract
- The effect of various peptide antagonists on capsaicin-induced (250 micrograms per ear) ear inflammation has been examined. 2. Co-administration of the substance P (SP) antagonist [D-Pro2,D-Trp7,9]SP at 100 and 300 micrograms per ear with capsaicin markedly attenuated oedema, whereas a vasopressin antagonist was ineffective. 3. Using the same scheme, the mixed BK2 and BK1 bradykinin (BK) antagonist NPC 567 (D-Arg[Hyp3,D-Phe7]BK) did not inhibit oedema at 100 micrograms per ear, but did inhibit at a higher dose (300 micrograms). The BK1 antagonist [Leu8,desArg9]BK produced significant inhibition at both doses. 4. When BK was used to induce ear inflammation (30 micrograms per ear), the SP antagonist inhibited ear oedema. Both BK receptor subtype antagonists inhibited inflammation with the BK1 being more potent than the BK2 antagonist. 5. These results suggest that BK1 along with BK2 receptors are located on capsaicin-sensitive fibres, where they may modulate the degree of neurogenic inflammation.
摘要
- 已研究了各种肽拮抗剂对辣椒素（每耳250微克）诱导的耳部炎症的影响。2. 每耳100微克和300微克的P物质（SP）拮抗剂[D-脯氨酸2，D-色氨酸7，9]SP与辣椒素共同给药可显著减轻水肿，而血管加压素拮抗剂则无效。3. 使用相同方案，混合的BK2和BK1缓激肽（BK）拮抗剂NPC 567（D-精氨酸[Hyp3，D-苯丙氨酸7]BK）在每耳100微克时不抑制水肿，但在较高剂量（300微克）时可抑制。BK1拮抗剂[亮氨酸8，去精氨酸9]BK在两种剂量下均产生显著抑制作用。4. 当使用BK诱导耳部炎症（每耳30微克）时，SP拮抗剂抑制耳部水肿。两种BK受体亚型拮抗剂均抑制炎症，其中BK1比BK2拮抗剂更有效。5. 这些结果表明，BK1和BK2受体位于辣椒素敏感纤维上，它们可能在其中调节神经源性炎症的程度。
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