Table 4.
Compound | MW | Log D | RCY | Target | IC50 for HDACs | In Vivo Properties in Rodents | Reference |
---|---|---|---|---|---|---|---|
[11C]22 | 375.42 | 1.8 | 25% | Class I | HDAC1: 60 nM HDAC2: 153 nM |
Brain uptake: <0.10% ID/cm3 after 3 min Metabolism: 80% of radioactivity in the brain was unchanged [11C]22 (rat) |
[101,105] |
[11C]23 | 268.30 | 1.0 | 10–15% | Class I | HDAC1: 45 nM HDAC2: 31 nM HDAC3: 20 nM |
– | [105] |
[11C]24 | 344.45 | 2.1 | 40% | Class I | HDAC1: 10 nM HDAC2: 20 nM |
– | [105] |
MW: molecular weight; RCY: radiochemical yield (decay corrected).