The anandamide transport inhibitor AM404 activates vanilloid receptors
The anandamide transport inhibitor AM404 activates vanilloid receptors
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DOI：
10.1016/s0014-2999(00)00207-7
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发表时间：
2000-05-12
影响因子：
5
通讯作者：
Högestätt, ED
中科院分区：
文献类型：
--
作者：
Zygmunt, PM;Chuang, HH;Högestätt, ED
大麻素转运抑制剂 N-(4-羟苯基)-5,8,11,14-二十碳四烯酰胺 (AM404) 结构与香草酸受体激动剂大麻素和辣椒素相似，也可能激活香草素受体并引起血管舒张。 AM404 在用去氧肾上腺素收缩的大鼠离体肝动脉段中引起浓度依赖性松弛。用辣椒素预处理的制剂消除了松弛。降钙素基因相关肽 (CGRP) 受体拮抗剂 CGRP-(8-37) 也消除了松弛。在表达香草酸亚型 1 受体 (VRI) 的非洲爪蟾卵母细胞膜片钳实验中，香草酸受体拮抗剂辣椒西平可抑制 AM404 引起的血管舒张，并阻断 AM404 诱导的电流。总之，AM404 激活天然和克隆的香草酸受体。 (C) 2000 Elsevier Science B.V. 保留所有权利。
The possibility that the anandamide transport inhibitor N-(4-hydroxyphenyl)-5,8,11,14-eicosatetraenamide (AM404), structurally similar to the vanilloid receptor agonists anandamide and capsaicin, may also activate vanilloid receptors and cause vasodilation was examined. AM404 evoked concentration-dependent relaxations in segments of rat isolated hepatic artery contracted with phenylephrine. Relaxations were abolished in preparations pre-treated with capsaicin. The calcitonin-gene related peptide (CGRP) receptor antagonist CGRP-(8-37) also abolished relaxations. The vanilloid receptor antagonist capsazepine inhibited vasodilation by AM404 and blocked AM404-induced currents in patch-clamp experiments on Xenopus oocytes expressing the vanilloid subtype 1 receptor (VRI). In conclusion, AM404 activates native and cloned vanilloid receptors. (C) 2000 Elsevier Science B.V. All rights reserved.