N-isopropyl-[123I] p-iodoamphetamine: single-pass brain uptake and washout; binding to brain synaptosomes; and localization in dog and monkey brain.
N-isopropyl-[123I] p-iodoamphetamine: single-pass brain uptake and washout; binding to brain synaptosomes; and localization in dog and monkey brain.
复制标题
N-异丙基-[123I]对碘苯丙胺：单次脑摄取和清除；
DOI：
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发表时间：
1980
影响因子：
9.3
通讯作者：
H. Parker
中科院分区：
文献类型：
--
作者：
H. S. Winchell;W. Horst;L. Braun;W. Oldendorf;R. Hattner;H. Parker
通过测定大鼠颈动脉注射后脑摄取指数(BUI)，测定了N-异丙基-对-[123I]碘苯丙胺在大鼠脑内的动力学，研究了N-异丙基-对-[123I]碘苯丙胺对大鼠脑皮质突触体内摄取和释放的影响，以及在狗和猴体内的分布。串联BUI对应于100%的第一次通过提取效率和大约318秒的洗脱半时间。S-(+)-异构体对突触体内去甲肾上腺素摄取的抑制作用与D-苯丙胺相当，但对突触体摄取5-羟色胺的抑制作用更强。两种异构体在引起突触体释放5-羟色胺方面都与D-苯丙胺相当，但S-(+)-异构体促进多巴胺释放，而D-苯丙胺不促进。未见犬脑核团的特异性定位，但在眼内有进行性堆积。在注射氯胺酮镇静剂的猴子中，注意到最初的大脑快速摄取，在接下来的20分钟内，大脑摄取进一步缓慢，但没有视网膜定位。高水平的大脑活动被维持了几个小时。该试剂在大脑中的定量初始单程清除表明它在评估局部脑血流灌注中的应用。它与脑胺结合部位的相互作用提示它可能在脑胺代谢研究中的应用。
The kinetics of N-isopropyl-p-[123I]iodoamphetamine in rat brains were determined by serial measurements of brain uptake index (BUI) after intracarotid injection; also studied were its effects on amine uptake and release in rat's brain cortical synaptosomes; and its in vivo distribution in the dog and monkey. Serial BUI correspond to a first-pass extraction efficiency of 100% and a washout half-time of approximately 318 sec. The S-(+)-isomer inhibited norepinephrine uptake in synaptosomes as strongly as D-amphetamine, but was more potent in inhibiting synaptosomal uptake of serotonin. Both isomers were comparable to D-amphetamine in causing release of serotonin from synaptosomes, but the S-(+)-isomer promoted release of dopamine, whereas D-amphetamine did not. No specific localization in brain nuclei of the dog was seen, but there was progressive accumulation in the eyes. Rapid initial brain uptake in the ketamine-sedated monkey was noted, and further slow brain uptake occurred during the next 20 min but without retinal localization. High levels of brain activity were maintained for several hours. The quantitative initial single-pass clearance of the agent in the brain suggests its use in evaluation of regional brain perfusion. Its interaction with brain amine-binding sites suggests its possible application in studies of cerebral amine metabolism.