A fundamental study on Emission CT receptor mapping by receptor autoradiography

受体放射自显影发射CT受体作图的基础研究

• 批准号: 63570488
• 负责人: MORI Hirofumi
• 金额: $ 0.77万
• 依托单位: Kanazawa University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for General Scientific Research (C)
• 财政年份: 1988
• 资助国家: 日本
• 起止时间: 1988 至 1989
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-63570488/
• 关键词: Autoradiography; Receptor; Neurotransmitter; Emission CT; Radioactive Ligand; Tecnetium-99m; Local Cerebral Blood Flow; オートラジオグラフィ; レセプター

Highly qualified autoradiograms were obtained using seven different ligands labeled with ^3H after the investigation of appropriate incubation time and washing time, and of presence or absence of saturation. The excellent spatial resolution of the recepter autoradiography, unlike the in vitro receptor assay, made it possible to compare the values for Bmax and Kd among the fine structures in the rat brain. Binding of ^3H-Katanserin to frontal lobe of the brain was significantly diminished in the Chlosipramine administered rats, white administration of haloperidol(HPD)failed to change the binding of ^3H-Spiperone in the rat brain.The effects of acute or chronic HPD administration on the local cerebral blood flow(LCBF) were measured by means of the quantitative autoradiographic technique. After acute HPD administration, the LCBF increased in the n.habenula and decreased in the medial frontal cortex. Chronic HPD administration reduced LCBF in the substantia nigra and ventral tegmental area, and increased LCBF in the n.caudatus-putamen and n.accumbens.We established a new method for the preparation of N-functionalized diaminodithiol for bifunctional chelating agents. The diaminodithiol prepared by our new method has high chelating ability of Te-99m and high stability of Tc-99m,and appears to be an attractive candidate as a useful chelator for bifunctional chelating agents.

在考察合适的孵育时间和洗涤时间以及是否存在饱和后，使用7种不同的配体标记了^3H，获得了高质量的自射线图。与体外受体测定不同，受体放射自显像具有良好的空间分辨率，可以比较大鼠脑内精细结构的Bmax和Kd值。氯丙嗪组大鼠脑额叶的^ 3h -卡坦色林结合明显减少，氟哌啶醇（HPD）未改变^3H-Spiperone在大鼠脑中的结合。采用定量放射自显像技术测定急性或慢性HPD给药对局部脑血流量（LCBF）的影响。急性HPD给药后，缰核LCBF增加，内侧额叶皮质LCBF减少。慢性给药可使大鼠黑质和腹侧被盖区LCBF减少，尾状核-壳核和伏隔核LCBF增加。该方法制备的二氨基二硫醇对Te-99m具有较高的螯合能力，对Tc-99m具有较高的稳定性，有望作为一种有用的双功能螯合剂。

项目成果

森厚文: "受容体オ-トラジオグラフィによるエミッションCT・レセプタ-マッピング" Innervision. 4. 47-49 (1989)

Atsufumi Mori：“使用受体放射自显影的发射 CT 和受体绘图”Innervision 4. 47-49 (1989)。

Hirofumi Mori: "Distribution of effects of haloperiodol on regional cerebral blood flow and D_2 receptor in the rat brain" J Cereb Blood Flow Metabol. 9. S138 (1989)

Hirofumi Mori：“卤代周期醇对大鼠大脑局部脑血流和 D_2 受体的影响分布”J Cereb Blood Flow Metabol。

Hirofumi Mori: "Characterization of the binding of N-isopropyl-p-[1-125]iodoamphetamine in the rat brain synaptosomal membranes" Nucl Med Communications.

Hirofumi Mori：“大鼠脑突触体膜中 N-异丙基-p-[1-125]碘苯丙胺结合的表征”Nucl Med Communications。

森厚文: INNERVISION. 6月号. (1989)

森厚文：INNERVISION 6 月号（1989 年）。

Hirofumi Mori: "Distribution of effects of haloperidol on regianol cerebral blood flow and D_2 receptor in the rat brain" J Cereb Blood Flow Metabol, 9 : P138, 1989.

Hirofumi Mori：“氟哌啶醇对大鼠大脑中 regianol 脑血流和 D_2 受体的影响分布”J Cereb Blood Flow Metabol，9：P138，1989。