Ikezaki K, Black K L, Santori E M, Smith M L, Becker D P, Payne B A, Toga A W
Division of Neurosurgery, Jonsson Cancer Center, Los Angeles, California.
Neurosurgery. 1990 Jul;27(1):78-82. doi: 10.1097/00006123-199007000-00011.
Experiments were undertaken to determine the in vivo utility of the mixed benzodiazepine ligand [3H]flunitrazepam and the selective peripheral benzodiazepine ligand [3H]PK 11195 [1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide] to outline the borders of rat C6 glial tumors in three dimensions. Intravenous injection of [3H]flunitrazepam resulted in a tumor/cortex ratio of radioactive densities between 2.7 and 1.5 within the first 60 minutes after injection. [3H]PK 11195 demonstrated a higher tumor/cortex ratio (5.3) than [3H]flunitrazepam. For three-dimensional studies, images were generated from thionin-stained histological sections and autoradiograms. The mixed type benzodiazepine ligand [3H]flunitrazepam was superior in showing some of the normal anatomical structures surrounding the tumor, whereas [3H]PK 11195, a specific peripheral ligand, demonstrated higher tumor/brain contrast and superior topographical correlation between histological and autoradiographic images. Implications of peripheral benzodiazepine receptor ligands for positron emission tomography are discussed.
开展了实验以确定混合苯二氮䓬配体[3H]氟硝西泮和选择性外周苯二氮䓬配体[3H]PK 11195[1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺]在体内勾勒大鼠C6胶质细胞瘤三维边界的效用。静脉注射[3H]氟硝西泮后，在注射后的前60分钟内，肿瘤/皮质放射性密度比在2.7至1.5之间。[3H]PK 11195显示出比[3H]氟硝西泮更高的肿瘤/皮质比(5.3)。对于三维研究，图像是从硫堇染色的组织学切片和放射自显影片生成的。混合型苯二氮䓬配体[3H]氟硝西泮在显示肿瘤周围一些正常解剖结构方面更具优势，而特异性外周配体[3H]PK 11195则显示出更高的肿瘤/脑对比度以及组织学和放射自显影图像之间更好的地形相关性。讨论了外周苯二氮䓬受体配体对正电子发射断层扫描的意义。
