346691-88-1Relevant articles and documents
Cross-coupling of [11C]methyllithium for 11C-labelled PET tracer synthesis
Helbert, Hugo,Antunes, Ines Farinha,Luurtsema, Gert,Szymanski, Wiktor,Feringa, Ben L.,Elsinga, Philip H.
supporting information, p. 203 - 206 (2021/01/13)
The cross-coupling of aryl bromides with [11C]CH3Li for the labelling of a variety of tracers for positron emission tomography (PET) is presented. The radiolabelled products were obtained in excellent yields, at rt and after short reaction times (3-5 min) compatible with the half-life of 11C (20.4 min). The automation of the protocol on a synthesis module is investigated, representing an important step towards a fast method for the synthesis of 11C-labelled compounds for PET imaging. This journal is
Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents.
Mathis, Chester A,Wang, Yanming,Holt, Daniel P,Huang, Guo-Feng,Debnath, Manik L,Klunk, William E
, p. 2740 - 2754 (2007/10/03)
The synthesis and evaluation of a series of neutral analogues of thioflavin-T (termed BTA's) with high affinities for aggregated amyloid and a wide range of lipophilicities are reported. Radiolabeling with high specific activity [(11)C]methyl iodide provided derivatives for in vivo evaluation. Brain entry in control mice and baboons was high for nearly all of the analogues at early times after injection, but the clearance rate of radioactivity from brain tissue varied by more than 1 order of magnitude. Upon the basis of its rapid clearance from normal mouse and baboon brain tissues, [N-methyl-(11)C]2-(4'-methylaminophenyl)-6-hydroxybenzothiazole (or [(11)C]6-OH-BTA-1) was selected as the lead compound for further evaluation. The radiolabeled metabolites of [(11)C]6-OH-BTA-1 were polar and did not enter brain. The binding affinities of [N-methyl-(3)H]6-OH-BTA-1 for homogenates of postmortem AD frontal cortex and synthetic Abeta(1-40) fibrils were similar (K(d) = 1.4 nM and 4.7 nM, respectively), but the ligand-to-Abeta peptide binding stoichiometry was approximately 400-fold higher for AD brain than Abeta(1-40) fibrils. Staining of AD frontal cortex tissue sections with 6-OH-BTA-1 indicated the selective binding of the compound to amyloid plaques and cerebrovascular amyloid. The encouraging in vitro and in vivo properties of [(11)C]6-OH-BTA-1 support the choice of this derivative for further evaluation in human subject studies of brain Abeta deposition.
Novel probes for imaging amyloid: iodinated benzothiazole derivatives
Zhuang, Z. P.,Kung, M.-P.,Hou, C.,Lee, C.-W.,Trojanowski, J. Q.,Lee, V. M.-Y.,Kung, H. F.
, p. S29 - S32 (2007/10/03)
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