Autoradiography of [3H]quipazine in rodent brain.

Autoradiography of [3H]quipazine in rodent brain.
复制标题

啮齿动物脑中[3H]奎帕嗪的放射自显影。

DOI:
10.1016/0014-2999(90)90342-4
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发表时间:
1990
影响因子:
5
通讯作者:
Perry,DC
Perry,DC
中科院分区:
医学2区
文献类型:
--
作者:
Perry,DC

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在大鼠脑切片中检查了[3 H]喹帕嗪结合位点的分布。该放射性配体已被证明在膜匀浆研究中标记5-HT 3受体。通过使用10 - 7 M ICS 205-930(一种高度选择性的5-HT 3拮抗剂)来定义非特异性结合,获得了[3 H]quipazine对这些受体的特异性。在髓质中检测到几个密集的5-HT 3特异性结合区域,最明显的是孤束核和三叉神经脊束尾侧部分。在梨状皮质、杏仁核后核、腹侧被盖区、嗅前核和上级丘等前脑区域,5-HT 3的结合水平呈低至中等水平。还对小鼠、沙鼠、仓鼠和豚鼠的脑切片进行了[3 H]奎帕嗪放射自显影。在这些物种的大部分大脑中,特异性结合相当低;然而,除豚鼠外,在所有动物的孤束核(以及小鼠的三叉神经脊束核)中均检测到密集的结合条纹。5-HT 3受体在脑中的分布可能有助于解释某些5-HT 3选择性药物的中枢神经系统活性。5-HT 3拮抗剂的止吐和镇痛作用可能是通过脑干感觉区的受体介导的。
The distribution of binding sites for [3H]quipazine was examined in sections from rat brain. This radioligand has been demonstrated to label 5-HT3receptors in membrane homogenate studies. Specificity of [3H]quipazine for these receptors was obtained by using 10−7M ICS 205-930, a highly selective 5-HT3antagonist, to define non-specific binding. Several areas of dense 5-HT3-specific binding were detected in the medulla, most notably the nucleus of the solitary tract and the caudal portion of the spinal trigeminal tract. Low to moderate levelsof 5-HT3binding were seen in several forebrain regions, including the pyriform cortex, posterior nuclei of the amygdala, ventral tegmental area, anterior olfactory nucleus and superior colliculus. [3H]Quipazine autoradiography was also performed on brain sections from mouse, gerbil, hamster and guinea pig. Specific binding was quite low throughout most of the brains from these species; however, in all but the guinea pig, dense streaks of binding were detected in nucleus of the solitary tract (and in the mouse, the nucleus of the spinal tract of the trigeminal nerve). The distribution of 5-HT3receptors in the brain may help explain some of the proposed CNS activities of 5-HT3-selective drugs. The anti-emetic and antinociceptive activities of 5-HT3antagonists may be mediated by receptors in the sensory areas in the brainstem.
5-HT3 受体拮抗剂 GR38032F 对向大鼠大脑腹侧被盖区注射神经激肽激动剂的反应的影响。
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发表时间: 1987
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发表时间: 1989
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发表时间: 1987
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DOI: --
发表时间: 1985
期刊:
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DOI: --
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