Inhibition of [3H]norepinephrine uptake in organ cultured rat superior cervical ganglia by xylamine.
Inhibition of [3H]norepinephrine uptake in organ cultured rat superior cervical ganglia by xylamine.
复制标题
木胺抑制器官培养大鼠颈上神经节对[3H]去甲肾上腺素的摄取。
DOI：
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发表时间：
1982
影响因子：
3.5
通讯作者：
A. Cho
中科院分区：
文献类型：
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作者：
J. Fischer;A. Cho
在器官培养中，大鼠的颈上神经节（SCG）在前2天显示出[3H]去甲肾上腺素（NE）摄取增加，然后在培养的第6天趋于平稳。培养的SCG对[3H]NE的摄取依赖于Na+和温度，并被可卡因、地西帕明和苯托品抑制，其抑制作用与报道的去甲肾上腺素能神经末梢的摄取抑制作用相似。该制剂也积累了[3H]多巴胺（DA），但是，与脑内NE和DA的摄取相反，地西帕明和苯托品对特定儿茶酚胺没有特异性，抑制[3H]NE和[3H]DA的摄取，其抑制作用与脑内NE摄取的作用相似。因此，观察到的DA摄取和SCG似乎主要通过NE摄取系统发生，而不是特定的DA摄取系统。10微米浓度的木胺（n -2-氯乙基- n -乙基-2-甲基苄胺）在30分钟内不可逆地抑制培养SCG对[3H]NE的摄取85%，在洗去未结合的药物后测量摄取。抑制的IC50约为0.3微米。当暴露于木胺后再次培养SCG时，[3H]NE摄取在2天后恢复。这种恢复被环己亚胺部分阻断，表明可能涉及新的摄取位点的合成。
The superior cervical ganglia (SCG) of the rat, when maintained in organ culture, show an increase in [3H]norepinephrine (NE) uptake in the first 2 days and then a leveling off of this activity through 6 days of culture. The [3H]NE uptake in cultured SCG is Na+ - and temperature-dependent and is inhibited by cocaine, desipramine and benztropine with potencies similar to those reported for uptake inhibition into noradrenergic nerve terminals. The preparation also accumulates [3H]dopamine (DA), but, in contrast to NE and DA uptake in the brain, desipramine and benztropine show no specificity for a particular catecholamine, inhibiting both [3H]NE and [3H]DA uptake with potencies similar to those shown for NE uptake in brain. Thus, observed DA uptake and SCG appears to occur mostly via the NE uptake system, not a specific DA uptake system. Xylamine (N-2-chloroethyl-N-ethyl-2-methylbenzylamine) at 10 microM irreversibly inhibits [3H]NE uptake in cultured SCG by 85% in 30 min, uptake being measured after washing away unbound drug. The IC50 for inhibition is about 0.3 microM. When SCG are again cultured after xylamine exposure, [3H]NE uptake recovers after 2 days. This recovery is partially blocked by cycloheximide, indicating that the synthesis of new uptake sites may be involved.