Department of Psychiatry and Division of Molecular Imaging and Neuropathology, Columbia University Medical Center and New York State Psychiatric Institute (NYSPI), New York, NY 10032, USA.
Int J Toxicol. 2011 Dec;30(6):611-8. doi: 10.1177/1091581811419024. Epub 2011 Oct 12.
Sprague Dawley rats (10/sex/group) were given a single intravenous (iv) dose of CUMI-101 to determine acute toxicity of CUMI-101 and radiation dosimetry estimations were conducted in baboons with [(11)C]CUMI-101. Intravenous administration of CUMI-101 did not produce overt biologically or toxicologically significant adverse effects except transient hypoactivity immediately after dose in the mid- and high-dose groups, which is not considered to be a dose-limiting toxic effect. No adverse effects were observed in the low-dose group. The no observed adverse effect level (NOAEL) is considered to be 44.05 µg/kg for a single iv dose administration in rats. The maximum tolerated dose (MTD) was estimated to be 881 µg/kg for a single iv dose administration. The Medical Internal Radiation Dose (MIRDOSE) estimates indicate the maximum permissible single-study dosage of [(11)C]CUMI-101 in humans is 52 mCi with testes and urinary bladder as the critical organ for males and females, respectively.
Sprague Dawley 大鼠（每组 10 只，雌雄各半）单次静脉注射 CUMI-101，以确定 CUMI-101 的急性毒性，并用 [(11)C]CUMI-101 对狒狒进行辐射剂量估算。静脉注射 CUMI-101 不会产生明显的生物学或毒理学不良反应，除了中高剂量组在给药后立即出现短暂的活动减少，但这不被认为是剂量限制毒性效应。低剂量组未观察到不良反应。单次静脉注射的无观察不良效应水平（NOAEL）被认为是 44.05 µg/kg。单次静脉注射的最大耐受剂量（MTD）估计为 881 µg/kg。医用内照射剂量（MIRDOSE）估计表明，[(11)C]CUMI-101 在单次研究中的最大允许剂量为 52 mCi，对于男性和女性，睾丸和膀胱分别为关键器官。
