Wakade A R
Br J Pharmacol. 1980 Jan;68(1):93-8. doi: 10.1111/j.1476-5381.1980.tb10703.x.
1 The noradrenaline (NA) content of various peripheral sympathetic neuroeffector organs and brain was measured at various times after different doses of reserpine administered to the rat.2 About a 25% reduction in the NA content of the heart was observed 24 h after 0.005 mg/kg reserpine. Two to ten times more reserpine was needed to obtain an approximately similar degree of depletion in the salivary gland and vas deferens; 0.1 mg/kg produced almost complete depletion in the heart and salivary gland, whereas 5 mg/kg was needed to deplete the vas deferens of its NA content.3 The NA content of the brain and superior cervical ganglion was lowered by 20 to 30% in 24 h only when the reserpine dose was raised to 0.1 mg/kg, and 5 to 10 mg/kg was required to obtain over 95% depletion.4 The rates of recovery of cardiac and salivary gland NA stores, after about 80 to 100% depletion by low and high doses of reserpine, were almost identical. About 50% restoration occurred in 7 to 15 days after a single dose of 0.1 mg/kg reserpine.5 The superior cervical ganglion, the NA content of which was fully depleted by 10 mg/kg, showed almost complete recovery in about 7 days.6 Transmural stimulation of the left atrium of the guinea-pig for 30 min (5 Hz for 30 s/min), or exposure of the atrium to reserpine (5 mug/ml) for 30 min, caused modest but statistically insignificant reduction in tissue NA content. However, stimulation in the presence of reserpine 5 mug/ml for 30 min produced about 50% depletion of NA.7In vitro reduction in NA content caused by reserpine plus transmural stimulation, was even more pronounced after treatment of the isolated vas deferens of the rat with tetraethylammonium.8 It is suggested that different rates of depletion following in vivo administration of reserpine are mainly due to variation in neuronal activity of different sympathetic neuroeffector organs.
给大鼠注射不同剂量的利血平后，在不同时间测量了各种外周交感神经效应器器官和大脑中的去甲肾上腺素（NA）含量。
给予0.005mg/kg利血平24小时后，观察到心脏中的NA含量降低了约25%。唾液腺和输精管需要2到10倍剂量的利血平才能达到大致相同程度的耗竭；0.1mg/kg可使心脏和唾液腺几乎完全耗竭，而输精管中NA含量耗竭则需要5mg/kg。
仅当利血平剂量提高到0.1mg/kg时，大脑和颈上神经节中的NA含量在24小时内降低20%至30%，需要5至10mg/kg才能实现超过95%的耗竭。
低剂量和高剂量利血平使心脏和唾液腺NA储备耗竭约80%至100%后，其恢复速率几乎相同。单次给予0.1mg/kg利血平后，7至15天内约有50%恢复。
颈上神经节，其NA含量在给予10mg/kg后完全耗竭，在约7天内几乎完全恢复。
对豚鼠左心房进行30分钟的跨壁刺激（5Hz，每分钟30秒），或使心房暴露于利血平（5μg/ml）30分钟，导致组织NA含量有适度但无统计学意义的降低。然而，在5μg/ml利血平存在下刺激30分钟导致约50%的NA耗竭。
利血平加跨壁刺激在体外导致的NA含量降低，在用四乙铵处理大鼠离体输精管后更为明显。
提示利血平体内给药后不同的耗竭速率主要是由于不同交感神经效应器器官的神经元活动差异所致。
