Ability of a new antitumor agent, AZQ, to penetrate into cerebrospinal fluid.
The ability of a new antitumor agent, AZQ (2,5-diaziridinyl-3,6-bis-carboethoxyamino-1,4-benzoquinone), NSC No. 182986, to enter the cerebrospinal fluid (CSF) was studied in nonhuman primates. Following parenteral administration of 14C-AZQ, CSF radioactivity rose quickly and reached a maximum value 60 min after administration. Total radioactivity in the CSF was about 25-35% of the corresponding plasma level at time points subsequent to maximum CSF concentration. Chloroform extraction and thin-layer chromatography revealed that much of the total radioactivity was not parent AZQ and that parent AZQ declined rapidly in both plasma and CSF with a half-life less than 1 h. AZQ clearly entered the CSF and yielded CSF concentrations comparable to plasma values.
D000818:Animals; D000970:Antineoplastic Agents / Q000097:blood / Q000134:cerebrospinal fluid*; D001388:Aziridines / Q000097:blood / Q000134:cerebrospinal fluid*; D001389:Azirines / Q000134:cerebrospinal fluid*; D016227:Benzoquinones; D008253:Macaca mulatta; D013997:Time Factors
D000970:Antineoplastic Agents; D001388:Aziridines; D001389:Azirines; D016227:Benzoquinones; C029108:diaziquone