title: [Carbon-11 labeled diacylglycerol for signal transduction imaging: effect of the solubilizer on the distribution and radiation dosimetry].
abstract: Carbon-11 labeled diacylglycerol (11C-DAG) has been developed as a signal transduction imaging agent for the CNS, and it can visualize the second messenger. For clinical application by positron CT (PET), the 11C-DAG solution must be prepared for intravenous injection. However, the 11C-DAG does not dissolve in water because of its lipophilicity and requires a solubilizer such as human serum albumin (HSA) and Tween 80 (TW-80). We examined the influence of these solubilizers on the tissue distribution of 11C-DAG, and estimated the radiation dosimetry. In the brain, uptake of 11C-DAG dissolved with HSA was 1.3-1.8 times higher than that of dissolved with TW-80. On the other hand, the lung and spleen showed a higher uptake of 11C-DAG using TW-80 than when using HSA. Especially, the lungs showed 20-40 times higher uptake than when using HSA. Also, the washout of radioactivity from tissue was slower, and the dose of radiation exposure was estimated to be higher, with TW-80 than with HSA. Therefore, between TW-80 and HSA with different solubilizing mechanisms, the later was suggested to be a better solubilizer of 11C-DAG.
authors.affiliation: Nishijin Hospital.
authors.forename: R
authors.initials: R
authors.lastname: Fujii
authors.forename: Y
authors.initials: Y
authors.lastname: Imahori
authors.forename: T
authors.initials: T
authors.lastname: Ido
authors.forename: K
authors.initials: K
authors.lastname: Wakita
authors.forename: H
authors.initials: H
authors.lastname: Horii
authors.forename: T
authors.initials: T
authors.lastname: Yagyu
authors.forename: N
authors.initials: N
authors.lastname: Higashi
authors.forename: H
authors.initials: H
authors.lastname: Mabuchi
authors.forename: Y
authors.initials: Y
authors.lastname: Ohmori
authors.forename: S
authors.initials: S
authors.lastname: Ueda
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D004075:Diglycerides / Q000493:pharmacokinetics; D006801:Humans; D011136:Polysorbates / Q000494:pharmacology*; D011874:Radiometry; D015290:Second Messenger Systems; D012709:Serum Albumin / Q000494:pharmacology*; D015398:Signal Transduction; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D004075:Diglycerides; D011136:Polysorbates; D012709:Serum Albumin