Table 1.
Radiolabeling and PET imaging application of CB1R specific tracers
| Radioligand (RCYs) | PET imaging study |
|
|---|---|---|
| subject | brain uptake | |
| [11c]5 (16±5%a) |
Rodents:obesity (myocardial imaging) NHP Human: SZ; obesity (myocardial imaging); alcohol dependence |
Mouse: 6.6 %ID/g (striatum, 15 min) Baboon: BP: 1.3 (putamen) Human: VT: 1.35±0.35 Human: SUVmax = 1.75±0.35 (putamen) Human: VT: 0.72±0.07 (putamen) |
| [11C]6 (2.5%±1.1 %b) | Rodents, NHP Human: SZ | Monkey: VT: 24.3 (mL/m3, striatum) Human: VT: 29.1±17.4 (putamen) Human: SUVmax= 3.5±0.5 (putamen) |
| [11C]7 (16.5%b) | Rodents, NHP | Rat: high BBB permeability, high specificity to CB1R Monkey: SUVmax = 3.3 (30 min) |
| [18F]8 (7.92±2.16%b) | Rodents, NHP | Rat: high BBB permeability, high specificly to CB1R Monkey: SUVmax = 2.75±0.75 (15 min) |
| [18F]9 (5.92%±1.34%b) | Rodents, NHP | Rat: high BBB permeability, high specificity to CB1IR Monkey: SUVmax = 5.75±0.75 (20 min) |
| [18F]10 (7.93±2.48%b) | Rodents: AD; BAT NHP Human: chronic cannabis smokers; alcohol-dependent; SZ; Psychosis |
Mouse: 1.5 %ID/mL (BAT) Monkey: SUVmax = 5.5±1.0 (20 min) Monkey: VT 35.4 (mL/m3, striatum) Human: SUVmax = 3.5±0.5 (putamen) Human: VT 24.3±7.2 (putamen) |
| [18F]11 (-) | Rodents: HD; PD NHP Human: anorexia and bulimia nervosa; episodic migraine; epilepsy; HD |
Rat, Monkey: high BBB permeability, high specificity to CB1R Human: SUVmax = 15±0.2 (putamen) Human: VT 25.1±13.3 (putamen) |
| [11C]12 (50%a) | Rodents, NHP, Human | Monkey: VT: 2.36 (mL/m3, striatum) Human: SUVmax = 2.35±0.65 (putamen) Human: VT: 3.15±0.70 (putamen) |
| [11C]15 (7.35±4.25%b) | NHP | Monkey: SUVmax = 2.2±0.5 (120 min) |
| [18F]16 (3.55±2.05%b) | NHP | Monkey: SUVmax = 1.8 (240 min) |
| [11C]7 (17±8%) | Rodents: BAT | Mouse: 2.8 %ID/mL (BAT) |
a
non-decay corrected RCYs
b
decay corrected RCYs
The data of PET imaging are listed only in the control group.