Campbell J A, Finn R D, Boothe T E, Djermouni B, Ginsberg M D, Lockwood A H, Gilson A J, Ache H J
J Nucl Med. 1981 Jun;22(6):538-41.
We have developed a method for the synthesis of C-11 iodoantipyrine. Carbon-11-labeled methyl iodide, prepared from 11CO2, was used to methylate 3-methyl-1-phenyl-2-pyrazolin-5-one to form C-11 antipyrine. Following silica-gel column chromatography and iodination, radiochemical purity of the C-11 iodoantipyrine was more than 99.5%, with a 10% yield and a specific activity of 30 mCi/mumol. Preliminary animal studies showed complete cerebral extraction and local cerebral blood-flow values that were within 4.6% of those obtained using C-14 iodoantipyrine. The C-11 analog, with positron emission tomography, will facilitate local cerebral blood-flow studies in human subjects.
我们已经开发出一种合成碳-11碘安替比林的方法。由11CO2制备的碳-11标记的碘甲烷用于使3-甲基-1-苯基-2-吡唑啉-5-酮甲基化，以形成碳-11安替比林。经过硅胶柱色谱法和碘化后，碳-11碘安替比林的放射化学纯度超过99.5%，产率为10%，比活度为30 mCi/μmol。初步动物研究表明，其脑摄取完全，局部脑血流量值与使用碳-14碘安替比林获得的值相差在4.6%以内。碳-11类似物结合正电子发射断层扫描，将有助于在人类受试者中进行局部脑血流量研究。
