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目的:考察哪些受体参与了莫索尼定的瞬时升压作用。方法:雌性自发性高血压大鼠(SHR)采用乌拉坦麻醉。分别经静脉给予可乐定(3、10、30μg/kg)和莫索尼定(0.1、0.3、1.0 mg/kg),经侧脑室给予莫索尼定或经胃管给予莫索尼定(1.0、10.0 mg/kg).观察瞬时升压现象的发生情况;莫索尼定(0.3 mg/kg)静脉注射前预注射哌唑嚷(10.0μg/kg)、育亨宾(2.0 mg/kg)、酚妥拉明(0.2 mg/kg)、咪唑克生(1.0 mg/kg)或育亨宾+咪唑克生(2.0 mg/kg+1.0 mg/kg),观察莫索尼定瞬时升压作用的变化情况.确定α1受体、α2受体和Ⅰ_1-咪唑啉受体在莫索尼定瞬时升压中的作用。结果:在降压程度相当的情况下,静脉注射莫索尼定的瞬时升压作用比可乐定强大得多。莫索尼定的瞬时升压作用不受哌唑嗪的影响.但可被育亨宾、酚妥拉明或咪唑克生部分阻断,而被育亨宾+咪唑克生完全阻断。莫索尼定侧脑室和胃管给药不产生瞬时升压现象。结论:静脉注射莫索尼定引起的瞬时升压作用是由外周α2受体和Ⅰ_1-咪唑啉受体共同介导的。
OBJECTIVE: To investigate which receptors are involved in the instantaneous boosting effect of moxonidine. Methods: Female spontaneously hypertensive rats (SHR) were anesthetized with urethane. Clonidine (3, 10, 30μg / kg) and moxonidine (0.1,0.3,1.0 mg / kg) were given intravenously, and moxonidine given intracerebroventricularly / kg) .Studies on the occurrence of instantaneous boost were observed. Pretreatment with moxonidine (0.3 mg / kg) was preconditioned with prazosin (10.0 μg / kg), yohimbine (2.0 mg / (0.2 mg / kg), midazolam (1.0 mg / kg) or yohimbine + midazolam (2.0 mg / kg + 1.0 mg / kg) to observe the changes of the instantaneous boosting effect of moxonidine. The Role of α1 Receptor, α2 Receptor and I_1-Imidazoline Receptors in Moxonidine Potentiation. RESULTS: Instantaneous vasopressors of intravenous moxonidine were much more potent than clonidine at comparable levels of depressurization. Moxonidine’s transient boost was not affected by prazosin, but partially blocked by yohimbine, phentolamine or midazolam, and was completely blocked by yohimbine + midazolam. Moxonidine intraventricular and intraventricular administration does not produce instantaneous pressure. CONCLUSION: The instantaneous boost induced by intravenous Moxonidine is mediated by the peripheral α2 receptor and the I_1-imidazoline receptor.