Smith R V, Wilcox R E, Soine W H, Riffee W H, Baldessarini R J, Kula N S
Res Commun Chem Pathol Pharmacol. 1979 Jun;24(3):483-99.
Clinical use of the potent dopaminergic partial-agonist apomorphine (APO) in a wide variety of neuropsychiatric disorders is hampered by a lack of data concerning tissue/plasma levels following various routes of administration. In the present experiments, plasma levels were assessed at various times up to 4 hours after APO administration IV, IP, and PO to mice and rats. Plasma levels of total radioactivity after PO administration of [3H]-APO were 50 to 65% of those seen after IV administration, but brain levels were almost undetectable after PO administration. Organic solvent-extractable concentrations of tritium-labelled material after IV and IP administration of [3H]-APO to mice were significantly lower than the levels of total radioactivity, while after PO administration, these concentrations were minimal. Similar results were observed in rats following IV and PO administration of [3H]-APO.
强效多巴胺能部分激动剂阿扑吗啡（APO）在多种神经精神疾病中的临床应用因缺乏不同给药途径后的组织/血浆水平数据而受到阻碍。在本实验中，对小鼠和大鼠静脉注射、腹腔注射和口服APO后，在长达4小时的不同时间点评估血浆水平。口服[3H]-APO后，总放射性的血浆水平为静脉注射后的50%至65%，但口服给药后脑内水平几乎检测不到。对小鼠静脉注射和腹腔注射[3H]-APO后，有机溶剂可萃取的氚标记物质浓度显著低于总放射性水平，而口服给药后这些浓度极低。对大鼠静脉注射和口服[3H]-APO后观察到类似结果。
