The depressor and vasodilator effects of rutaecarpine are mediated by calcitonin gene-related peptide
The depressor and vasodilator effects of rutaecarpine are mediated by calcitonin gene-related peptide
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DOI：
10.1055/s-2003-37703
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发表时间：
2003-02-01
期刊：
影响因子：
2.7
通讯作者：
Li, YJ
中科院分区：
文献类型：
--
作者：
Hu, CP;Xiao, LA;Li, YJ
已有研究表明，吴茱萸次碱具有降压和扩血管作用，并激活香草酸受体引起降钙素基因相关肽（CGRP）释放。在本研究中，我们研究了吴茱萸次碱的降压和扩血管作用是否与通过激活香草酸受体刺激内源性CGRP释放有关。吴茱萸次碱（30、100或300 μ g/kg，i. v.）的辣椒碱（50 mg/kg，s. c.）会消耗感觉神经中的神经递质在主动脉和上级肠系膜动脉环中，吴茱萸次碱（10（-7）-10（-5）M）或辣椒素（3 × 10（-9）- 3 × 10（-6）M）引起浓度依赖性血管舒张反应，该反应可被辣椒平（10（-5）M）（一种竞争性香草素受体拮抗剂）或CGRP-（8 - 37）（10（-6）M）显著减弱，一种选择性CGRP受体拮抗剂。用辣椒素（10（-5）M）预处理20分钟后，对吴茱萸次碱的舒张反应也明显减弱。类似地，用吴茱萸次碱（10（-5）M）预处理20分钟也减弱辣椒素的血管舒张反应。这些结果表明，吴茱萸次碱的降压和扩血管作用与通过激活香草酸受体刺激内源性CGRP释放有关。
Previous studies have shown that rutaecarpine has depressor and vasodilator effects, and activates vanilloid receptors to evoke calcitonin gene-related peptide (CGRP) release. In the present study, we examined whether the depressor and vasodilator effects of rutaecarpine are related to the stimulation of endogenous CGRP release via activation of vanilloid receptors in rats. Rutaecarpine (30, 100, or 300 mug/kg, i. v.) caused a depressor effect concomitantly with an increase in the plasma concentrations of CGRP in a dose-dependent manner, and the effects of rutaecarpine were abolished by pretreatment with capsaicin (50 mg/kg, s. c.) which depletes neurotransmitters in sensory nerves. In aortic and superior mesenteric arterial rings, rutaecarpine (10(-7)-10(-5) M) or capsaicin (3 x 10(-9) - 3 x 10(-6) M) caused a concentration-dependent vasodilator response, which was significantly attenuated by capsazepine (10(-5) M), a competitive vanilloid receptor antagonist, or by CGRP-(8 - 37) (10(-6) M), a selective CGRP receptor antagonist. After pretreatment with capsaicin (10(-5) M) for 20 min, vasodilator responses to rutaecarpine were also markedly attenuated. Similarly, pretreatment with rutaecarpine (10(-5) M) for 20 min also attenuated vasodilator responses to capsaicin. These results suggest that the depressor and vasodilator effects of rutaecarpine are related to stimulation of endogenous CGRP release via activation of vanilloid receptors in rats.