del Carmen García María, Adler-Graschinsky Edda, Celuch Stella Maris
Cátedra de Farmacología, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Buenos Aires, Argentina.
Naunyn Schmiedebergs Arch Pharmacol. 2003 Oct;368(4):270-6. doi: 10.1007/s00210-003-0800-x. Epub 2003 Sep 18.
This study examined the effect of intrathecal (i.t.) injection of the endocannabinoid anandamide in urethane-anesthetized rats. The tip of the i.t. cannula was positioned at the T(12)-L(1) level of the spinal cord. Either anandamide or its metabolically stable analogue methanandamide (25 to 100 nmol) produced dose-dependent decreases in the blood pressure that persisted at least for up to 30 min. The hypotensive responses to 100 nmol anandamide and to 100 nmol methanandamide were -17.7+/-1.6 mmHg ( n=5) and -17.9+/-2.0 mmHg ( n=4), respectively. Hypotensive effects were also obtained with the CB(1) cannabinoid receptor agonist WIN 55212-2 (20 nmol; i.t.) as well as with the vanilloid VR(1) receptor agonist capsaicin (3 nmol; i.t.). Nicotinic ganglionic blockade with hexamethonium bromide [10 mg/kg; intravenous(i.v.)] abolished the responses to both anandamide and capsaicin. The i.t. administration of the CB(1) receptor antagonist, 20 nmol SR 141716A, as well as the VR(1) receptor antagonist, 20 nmol capsazepine, prevented almost completely the hypotensive responses to both anandamide and methanandamide. SR 141716A prevented the hypotension caused by WIN 55212-2 but did not modify the response to the vanilloid receptor agonist capsaicin. On the contrary, capsazepine antagonized the hypotension caused by capsaicin but failed to affect the decrease in blood pressure caused by the CB1 cannabinoid receptor agonist WIN 55212-2. These results suggest that anandamide could modulate the blood pressure through the activation of cannabinoid CB(1) receptors and vanilloid VR(1) receptors localized at the spinal cord.
本研究检测了鞘内注射内源性大麻素花生四烯酸乙醇胺对氨基甲酸乙酯麻醉大鼠的影响。鞘内插管尖端置于脊髓胸12至腰1水平。花生四烯酸乙醇胺或其代谢稳定类似物甲烷花生四烯酸乙醇胺(25至100 nmol)可使血压呈剂量依赖性下降,且至少持续30分钟。对100 nmol花生四烯酸乙醇胺和100 nmol甲烷花生四烯酸乙醇胺的降压反应分别为-17.7±1.6 mmHg(n = 5)和-17.9±2.0 mmHg(n = 4)。CB1大麻素受体激动剂WIN 55212-2(20 nmol;鞘内注射)以及香草酸受体VR1激动剂辣椒素(3 nmol;鞘内注射)也可产生降压作用。用溴化六甲铵[10 mg/kg;静脉注射]进行烟碱样神经节阻断可消除对花生四烯酸乙醇胺和辣椒素的反应。鞘内注射CB1受体拮抗剂20 nmol SR 141716A以及VR1受体拮抗剂20 nmol辣椒平,几乎可完全阻止对花生四烯酸乙醇胺和甲烷花生四烯酸乙醇胺的降压反应。SR 141716A可阻止WIN 55212-2引起的低血压,但不改变对香草酸受体激动剂辣椒素的反应。相反,辣椒平可拮抗辣椒素引起的低血压,但未能影响CB1大麻素受体激动剂WIN 55212-2引起的血压下降。这些结果表明,花生四烯酸乙醇胺可通过激活位于脊髓的大麻素CB1受体和香草酸VR1受体来调节血压。