Paroxetine as an in vivo indicator of 3,4-methylenedioxymethamphetamine neurotoxicity: a presynaptic serotonergic positron emission tomography ligand?
Paroxetine as an in vivo indicator of 3,4-methylenedioxymethamphetamine neurotoxicity: a presynaptic serotonergic positron emission tomography ligand?
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帕罗西汀作为 3,4-亚甲二氧基甲基苯丙胺神经毒性的体内指标：突触前血清素能正电子发射断层扫描配体？
DOI：
10.1016/0006-8993(90)91064-n
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发表时间：
1990
期刊：
影响因子：
2.9
通讯作者：
Ricaurte,GA
中科院分区：
文献类型：
--
作者：
Scheffel,U;Ricaurte,GA
本研究旨在确定[3 H]帕罗西汀，一种有效的和选择性的抑制剂，5-羟色胺摄取在体外，可用于标记5-羟色胺转运体在大鼠大脑中的体内，这样它可能会被用来开发突触前多巴胺能正电子发射断层扫描配体。氚标记帕罗西汀通过尾静脉注射给药于大鼠。4小时后，通过从其他感兴趣的脑区域的总结合中减去小脑中的非特异性结合来确定特异性[3 H]帕罗西汀结合。特异性[3 H]帕罗西汀结合的分布与所有检查的脑区中5-羟色胺摄取位点的分布一致。用5-羟色胺再摄取抑制剂（西酞普兰或舍曲林）预处理可使体内特异性[3 H]帕罗西汀结合率降低99%。通过使用5，7-二羟基色胺（5，7-DHT）（一种已知的多巴胺能神经毒素）进一步表征了体内[3 H]帕罗西汀结合的特异性。5，7-DHT（200 μg，i.c.v.）引起特异性[3 H]帕罗西汀结合的显著减少，并引起局部脑5-羟色胺的长期消耗。在最后一项研究中，测试了使用体内[3 H]帕罗西汀结合作为另一种神经毒素（3，4-亚甲二氧基甲基苯丙胺，MDMA）诱导的多巴胺能损伤指标的可行性。MDMA处理的大鼠表现出体内[3 H]帕罗西汀结合的显著降低，沿着区域脑5-羟色胺的持久消耗。这些结果表明，[~ 3 H]帕罗西汀可用于标记大鼠脑内5-羟色胺摄取位点，并可使用体内[~ 3 H]帕罗西汀结合作为指示剂来检测由多巴胺能神经毒素引起的损伤。因此，帕罗西汀（或其衍生物之一）有望作为PET配体，用于研究健康以及神经毒性损伤后的活体人脑中的多巴胺能神经元。
The present study sought to determine whether [3H]paroxetine, a potent and selective inhibitor of serotonin uptake in vitro, could be used to label the serotonin transporter in the rat brain in vivo such that it might be employed to develop a presynaptic serotonergic positron emission tomography ligand. Tritium labeled paroxetine was administered intravenously to rats by means of tail vein injection. Four hours later, specific [3H]paroxetine binding was determined by subtracting non-specific binding in the cerebellum from total binding in other brain regions of interest. The distribution of specific [3H]paroxetine binding paralleled the distribution of serotonin uptake sites in all brain regions examined. Pretreatment with serotonin re-uptake inhibitors (citalopram or sertraline) reduced in vivo specific [3H]paroxetine binding by as much as 99%. Specific in vivo [3H]paroxetine binding was further characterized through the use of 5,7-dihydroxytryptamine (5,7-DHT), a known serotonergic neurotoxin. 5,7-DHT (200 μg, i.c.v.) caused a marked reduction in specific [3H]paroxetine binding, and induced a prolonged depletion of regional brain serotonin. In a final study, the feasibility of using in vivo [3H]paroxetine binding as an indicator of serotonergic damage induced by another neurotoxin (3,4-methylenedioxymethamphetamine, MDMA) was tested. MDMA-treated rats showed a profound reduction in in vivo [3H]paroxetine binding, along with a lasting depletion of regional brain serotonin. These results demonstrate that [3H]paroxetine can be used to label serotonin uptake sites in rat rat brain in vivo, and that the damage induced by serotonergic neurotoxins can be detected using in vivo [3H]paroxetine binding as an indicator. Paroxetine (or one of its derivatives) therefore holds promise as a PET ligand for studying serotonergic neurons in the living human brain in health as well as after neurotoxic injury.
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DOI：
10.1176/ajp.145.8.937
发表时间：
1988-08
期刊：
The American journal of psychiatry
影响因子：
--
作者：
H. Mayberg;R. Robinson;D. Wong;Parikh Rm;P. Bolduc;S. Starkstein;T. Price;R. Dannals;J. Links;A. Wilson
通讯作者：
H. Mayberg;R. Robinson;D. Wong;Parikh Rm;P. Bolduc;S. Starkstein;T. Price;R. Dannals;J. Links;A. Wilson
[3H]帕罗西汀在大鼠脑中结合的表征
影响因子：
4.7
作者：
J. Marcusson;M. Bergstrom;K. Eriksson;S. Ross
通讯作者：
S. Ross
使用定量放射自显影技术研究 5, 7-二羟基色胺对整个大鼠中枢神经系统血清素 1 和血清素 2 受体的影响
影响因子：
2.9
作者：
C. Fischette;B. Nock;K. Renner
通讯作者：
K. Renner
血清素能功能的药理学修饰：用于研究和治疗精神疾病和其他疾病的药物。
DOI：
--
发表时间：
1986
期刊：
影响因子：
--
作者：
Fuller Rw
通讯作者：
Fuller Rw
中脑中缝损伤后离散脑区域的色氨酸羟化酶活性和突触体对血清素的摄取：与血清素水平和组织化学荧光的相关性。
影响因子：
2.9
作者：
M. Kuhar;G. Aghajanian;R. Roth
通讯作者：
R. Roth