el Dareer S M, Kalin J R, Tillery K F, Hill D L
Southern Research Institute, Birmingham, Alabama 35255-5305.
J Toxicol Environ Health. 1988;23(3):385-93. doi: 10.1080/15287398809531121.
The disposition of 2-(2-quinolyl)-1,3-indandione (D. C. yellow #11, DCY) in male Fischer rats dosed intravenously or by feeding was determined. For rats given [14C]DCY in the feed (0.00044-0.41% of the diet), recovery of radioactivity during the 24-h dosing period and the 72-h period thereafter ranged from 89.1 to 93.9% for feces and from 4.98 to 6.25 for urine. Tissues contained only trace amounts. Following intravenous dosing with [14C]DCY (0.93 mg/kg), radioactivity distributed readily into most tissues; maximum amounts were present at 5 min, the earliest time of assay. Maximum amounts of radioactivity in fat, skin, and gut tissue, however, were present at 30 min after dosing. These three tissues also had relatively long alpha phases for the elimination of radioactivity. In 24 h after intravenous dosing, rats excreted 81.1% of the dose in the feces and 16.0% of the dose in the urine. For rats fitted with biliary cannulas, 54.5% of the dose, all of which was metabolites of [14C]DCY, was recovered in the bile in 4 h. Associated with the rapid and extensive biliary excretion of metabolites of intravenously administered [14C]DCY was the appearance of large amounts of radioactivity in the feces and also, at intermediate time points, in the liver, gut contents, and gut tissue. In conclusion, rats rapidly distribute, metabolize, and excrete [14C]DCY.
测定了2-(2-喹啉基)-1,3-茚二酮（D.C.黄#11，DCY）在雄性Fischer大鼠静脉给药或经口给药后的处置情况。对于经口给予[14C]DCY（占饮食的0.00044 - 0.41%）的大鼠，在24小时给药期及随后的72小时内，粪便中放射性的回收率为89.1%至93.9%，尿液中为4.98%至6.25%。组织中仅含痕量。静脉注射[14C]DCY（0.93毫克/千克）后，放射性迅速分布到大多数组织中；在最早检测时间5分钟时达到最大量。然而，脂肪、皮肤和肠道组织中的放射性最大量在给药后30分钟出现。这三种组织在放射性消除方面也有相对较长的α相。静脉给药后24小时内，大鼠粪便中排出剂量的81.1%，尿液中排出剂量的16.0%。对于装有胆管插管的大鼠，4小时内胆汁中回收了剂量的54.5%，所有这些都是[14C]DCY的代谢产物。与静脉注射[14C]DCY代谢产物的快速和大量胆汁排泄相关的是，粪便中出现大量放射性，在中间时间点，肝脏、肠道内容物和肠道组织中也出现大量放射性。总之，大鼠能快速分布、代谢和排泄[14C]DCY。
