Potentiation of anandamide hypotension by the transport inhibitor, AM404

Potentiation of anandamide hypotension by the transport inhibitor, AM404
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DOI:
10.1016/s0014-2999(97)01297-1
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发表时间:
1997-10-15
影响因子:
5
通讯作者:
Piomelli, D
Piomelli, D
中科院分区:
医学2区
文献类型:
--
作者:
Calignano, A;LaRana, G;Piomelli, D

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推定的内源性大麻素 anandamide (0.2-2 mg/kp i.v.) 可以剂量依赖性地降低麻醉豚鼠的全身血压。 CBI 大麻素受体拮抗剂 SR141716A [N-(哌啶-1-基)-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-1H-吡唑-3-甲酰胺可防止这些影响。 HCl],剂量为 0.2 mg/kg,静脉注射。载体介导的 anandamide 转运的新型抑制剂 N-(4-羟苯基)花生四烯乙醇酰胺 (AM404)(10 mg/kg,静脉注射)显着增强和延长了对 anandamide 的血管抑制反应。这些结果表明 anandamide 转运参与终止 anandamide 的血管作用。 (C) 1997 Elsevier Science B.V.
The putative endogenous cannabinoid, anandamide (0.2-2 mg/kp i.v.), decreased systemic blood pressure dose-dependently in anesthesized guinea pigs. These effects were prevented by the CBI cennabinoid receptor antagonist SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide . HCl] at the dose of 0.2 mg/kg i.v. The vasodepressor responses to anandamide were significantly potentiated and prolonged by a novel inhibitor of carrier-mediated anandamide transport, N-(4-hydroxyphenyl) arachidonylethanolamide (AM404)(10 mg/kg, i.v.). These results suggest that anandamide transport participates in terminating the vascular actions of anandamide. (C) 1997 Elsevier Science B.V.