[Differential inhibition of raubasine and tetrahydroalstonine on the vasopressor response to sympathetic nervous stimulation and intravenous noradrenaline in the pithed rat].

Journal de pharmacologie Pub Date : 1985-10-01
J Roquebert, P Demichel, P Dufour
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Abstract

The effects of raubasine and tetrahydroalstonine (THA) on the vasopressor response to sympathetic nerve stimulation and to i.v. administration of noradrenaline were studied in the pithed rat to ascertain whether raubasine and THA would preferentially block pressor responses due to exogenous versus endogenous noradrenaline alpha-adrenergic receptor activation. Raubasine (0.5 to 4 mg/kg i.v.) was more effective in blocking the response due to sympathetic nerve stimulation than that due to i.v. noradrenaline. On the other hand THA (0.5 to 4 mg/kg i.v.) produced greater inhibition of the i.v. noradrenaline response than the sympathetic nerve stimulation response. THA (0.5, 1, 2 mg/kg i.v.) enhanced the nerve stimulation response, while at the 4 mg/kg dose the response was slightly reduced. This may be explained by a preferential block by THA at low doses, of presynaptic alpha 2-adrenoceptors. In pithed rat raubasine and THA showed dose-related blocking effects on the pressor response of phenylephrine and B-HT 933, respectively. This suggest that raubasine preferentially blocks alpha-1 and THA alpha 2-adrenoceptors. The results suggest that raubasine and THA preferentially block the pressor responses of post-synaptic alpha-adrenergic receptor activation due to endogenous and exogenous noradrenaline, respectively.

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[劳巴辛和四氢alstonine对大鼠交感神经刺激和静脉注射去甲肾上腺素的血管加压反应的差异抑制]。
我们研究了劳巴辛和四氢alstonine (THA)对交感神经刺激和静脉给药去甲肾上腺素的加压反应的影响,以确定劳巴辛和THA是否会优先阻断外源性和内源性去甲肾上腺素α -肾上腺素能受体激活引起的加压反应。紫荆碱(0.5 ~ 4mg /kg静脉注射)比去甲肾上腺素静脉注射更有效地阻断交感神经刺激引起的反应。另一方面,THA (0.5 ~ 4mg /kg静脉注射)对去甲肾上腺素静脉注射反应的抑制作用大于交感神经刺激反应。THA(0.5、1、2 mg/kg静脉注射)增强了神经刺激反应,而在4 mg/kg剂量下,反应略有降低。这可以解释为低剂量THA优先阻断突触前α 2-肾上腺素受体。在灌胃大鼠中,劳巴辛和THA分别对苯肾上腺素和B-HT 933的升压反应表现出剂量相关的阻断作用。这表明劳巴辛优先阻断α -1和THA α - 2肾上腺素受体。结果表明,raubasine和THA分别优先阻断内源性和外源性去甲肾上腺素引起的突触后α -肾上腺素能受体激活的压力反应。
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