APOMORPHINE-INDUCED EMESIS IN THE DOG - ROUTES OF ADMINISTRATION, EFFICACY AND SYNERGISM BY NALOXONE
APOMORPHINE-INDUCED EMESIS IN THE DOG - ROUTES OF ADMINISTRATION, EFFICACY AND SYNERGISM BY NALOXONE
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DOI：
10.1111/j.1365-2885.1990.tb00763.x
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发表时间：
1990-06-01
影响因子：
1.3
通讯作者：
FREY, HH
中科院分区：
文献类型：
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作者：
SCHERKL, R;HASHEM, A;FREY, HH
阿扑吗啡被证明是更有效的催吐剂在狗后s.c.给药后，i.m.注射剂量为0.04和0.1 mg/kg。这种作用由μ-α介导的止吐作用解释。化学感受器是大脑中呕吐中心的化学感受器，与化学感受器触发区相反，化学感受器触发区位于血脑屏障内。在化学感受器触发区中D2-受体的刺激（引起呕吐）和μ-受体之间的一定延迟。因此，呕吐中心的受体（产生止吐作用），导致自限性呕吐。封锁μ-纳洛酮可增强并延长阿扑吗啡的作用。皮下注射阿扑吗啡的浓度范围相对较窄。因此，给药有效地刺激化学感受器触发区，但几乎不能抑制呕吐中心，因此必须认为是阿扑吗啡给药的最合适途径。
Apomorphine proved to be more effective as an emetic in dogs after s.c. administration than after i.m. injection with doses of 0.04 and 0.1 mg/kg. This effect is explained by an anti-emetic effect mediated by .mu.-receptors in the vomiting centre in the brain, which, in contrast to the chemoreceptor trigger zone, is within the blood-brain barrier. A certain delay between the stimulation of D2-receptors in the chemoreceptor trigger zone (causing emesis) and .mu.-receptors in the vomiting centre (producing anti-emesis) therefore results, leading to a self-limiting emesis. Blockade of the .mu.-receptors by naloxone increased and prolonged the effect of apomorphine. A relatively narrow range of apomorphine concentrations on s.c. administration is then effective to stimulate the chemoreceptor trigger zone, but can hardly inhibit the vomiting centre, and must therefore be considered the most suitable route for administration of apomorphine.