Brannan T, Prikhojan A, Yahr M D
Department of Neurology, Mount Sinai School of Medicine, New York, NY, USA.
Brain Res. 1998 Feb 16;784(1-2):148-53. doi: 10.1016/s0006-8993(97)01191-8.
We tested the circling response to l-DOPA and apomorphine administration in rats with unilateral 6-hydroxydopamine (6-OHDA) lesions of the substantia nigra. Rats demonstrated a progressively diminished circling response when l-DOPA-carbidopa was repeatedly administered at 120 min intervals. This decreasing response was not present when apomorphine was administered under the same conditions. We also perfused l-DOPA directly into the striatum in vivo of rats with an ipsilateral 6-OHDA nigrotomy at 60 min intervals and monitored striatal dopamine levels with the technique of brain microdialysis. Dopamine formation increased from the first to the fifth trial. This may be secondary to the decrease in uptake sites which accompanies the loss of striatal dopamine nerve terminals. We postulate that the continued presence of dopamine at striatal receptor sites conditions a short-term loss of dopamine receptor sensitivity and a consequent decreased circling response. The observation that desensitization (as measured by decreasing circling) was not present following repeated apomorphine administration may be attributable to its shorter duration of action. We also perfused l-DOPA into the striatum of normal rats and noted a progressive decrease in striatal dopamine levels from the first to the fifth trial. Since this occurred following direct administration of l-DOPA into the striatum, the decrease could not be accounted for by peripheral pharmacodynamics or bioavailability of l-DOPA in the striatum. Since this decrease in dopamine formation was seen only in the normal striatum, its relevance to the diminished behavioral response is unclear.
我们在患有单侧黑质6-羟基多巴胺(6-OHDA)损伤的大鼠中测试了左旋多巴和阿扑吗啡给药后的转圈反应。当以120分钟的间隔重复给予左旋多巴-卡比多巴时,大鼠的转圈反应逐渐减弱。在相同条件下给予阿扑吗啡时,这种反应减弱并不存在。我们还以60分钟的间隔将左旋多巴直接灌注到同侧6-OHDA黑质切开术大鼠的纹状体中,并采用脑微透析技术监测纹状体多巴胺水平。从第一次试验到第五次试验,多巴胺生成增加。这可能继发于纹状体多巴胺神经末梢丧失伴随的摄取位点减少。我们推测,多巴胺在纹状体受体位点的持续存在导致多巴胺受体敏感性短期丧失,从而使转圈反应减弱。重复给予阿扑吗啡后未出现脱敏(通过转圈减少来衡量)这一观察结果可能归因于其作用持续时间较短。我们还将左旋多巴灌注到正常大鼠的纹状体中,并注意到从第一次试验到第五次试验纹状体多巴胺水平逐渐降低。由于这是在将左旋多巴直接注入纹状体后发生的,这种降低不能用左旋多巴在纹状体中的外周药效学或生物利用度来解释。由于仅在正常纹状体中观察到多巴胺生成的这种降低,其与行为反应减弱的相关性尚不清楚。