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INFORMATION FOR

PET Core Radioligands

Abbreviations

  • AD – Alzheimer’s Disease
  • PD – Parkinson Disease
  • MS – Multiple Sclerosis
  • HD – Huntington's Disease
  • NSCLC – Non-small cell lung cancer

PET Radioligands for Human use

Metabotropic receptor

TracerTargetExample Uses
[11C]ABP688
mGluR5 availability
AD
[18F]FPEB
Metabotropic glutamate mGluR5
PD, Fragile X Syndrome
[11C]CUMI-101
Serotonin 5-HT1A Receptor
Depression
11C]P943
Serotonin 5-HT1B Receptor
Depression
[11C]MDL100907
Serotonin 5-HT2A receptors
Schizophrenia
[11C]SB-207145
Serotonin 5-HT4 Receptor
AD, depression
[11C]GSK-215083
Serotonin 5-HT6 Receptor
AD, depression
[11C]PHNO
Dopamine D2/D3 antagonist
PD, addiction, schizophrenia
[11C]FLB457
Extrastriatal dopamine D2/D3
Depression
[11C]Raclopride
Dopamine D2/D3 antagonist
PD
[11C]Carfentanil
µ opiate receptor agonist
Pain, HD, PD
[11C]LY2795050
Kappa Opioid Antagonist Ligand
Addiction, depression
[18F]LY2459989
Kappa Opioid Receptor antagonist
Addiction, depression
[11C]GR103545
Kappa Opioid Receptor agonist
Addiction, depression
[11C]EKAP
Kappa Opioid Receptor agonist
Addiction, depression
[11C]LSN3172176
M1 muscarinic acetylcholine receptor
AD, PD
[11C]OMAR
Cannabinoid subtype 1 receptor
Neuropsychiatric disorders
[11C]GSK189254
Histamine H3 Receptor
Neuropsychiatric disorders
[11C]APM699
Vasopressin 1B Receptor (V1b)
Neuropsychiatric disorders
[11C]AM646
Lysophosphatidic Acid Receptor Type 1 (LPA1)
Lung Fibrosis
[18F]LPA327
Lysophosphatidic Acid Receptor Type 1 (LPA1)
Lung Fibrosis

Ionotropic receptor

Tracer
  • [18F]ASEM
  • [18F]NCFHEB ([18F]Flubatine)
  • [18F]GAT44
  • (S)-[18F]OF-NB1
Target
  • α7-nAChR
  • α4β2- Nicotinic acetylcholine receptors
  • γ-Aminobutyric acid (GABA)
  • NMDA
Example Uses
  • Schizophrenia, AD, PD
  • AD
  • Neurologic and psychiatric diseases
  • Neuropsychiatric disorders
[18F]ASEM
α7-nAChR
Schizophrenia, AD, PD
[18F]NCFHEB ([18F]Flubatine)
α4β2- Nicotinic acetylcholine receptors
AD
[18F]GAT44
γ-Aminobutyric acid (GABA)
Neurologic and psychiatric diseases
(S)-[18F]OF-NB1
NMDA
Neuropsychiatric disorders

Transporter target

Tracer
  • [18F]FE-PE2I
  • [11C]PE2I
  • [18F]FPDTBZ ([18F]AV133)
  • [11C]DASB
  • [11C]MRB
Target
  • Dopamine transporter (DAT)
  • Vesicular Monoamine Transporter (VMAT2)
  • Serotonin Transporter (SERT)
  • Norepinephrine transporters (NET)
Example Uses
  • PD
  • Depression
  • Drug occupancy studies
[18F]FE-PE2I
Dopamine transporter (DAT)
PD
[11C]PE2I
Dopamine transporter (DAT)
PD
[18F]FPDTBZ ([18F]AV133)
Vesicular Monoamine Transporter (VMAT2)
PD
[11C]DASB
Serotonin Transporter (SERT)
Depression
[11C]MRB
Norepinephrine transporters (NET)
Drug occupancy studies

Enzyme target

Tracer
  • [11C]MK-3168
  • [18F]Bavarostat
  • [11C]AS2471907
  • [18F]AS2471907
  • [18F]T401 (MGL401)
  • [18F]P247
Target
  • Fatty acid amide hydrolase
  • Histone Deacetylase-6 (HDAC6) inhibitor
  • 11β-HSD1
  • Monoacylglycerol lipase (MAGL)
Example Uses
  • FAAH availability for drug dose selection
  • PD, AD
  • Stress, cortisol
  • neuropsychiatric disorders
[11C]MK-3168
Fatty acid amide hydrolase
FAAH availability for drug dose selection
[18F]Bavarostat
Histone Deacetylase-6 (HDAC6) inhibitor
PD, AD
[11C]AS2471907
11β-HSD1
Stress, cortisol
[18F]AS2471907
11β-HSD1
Stress, cortisol
[18F]T401 (MGL401)
Monoacylglycerol lipase (MAGL)
neuropsychiatric disorders
[18F]P247
Monoacylglycerol lipase (MAGL)
neuropsychiatric disorders

Synaptic proteins

Tracer
  • [11C]UCB-J
  • [18F]SynVesT-1 (SDM8)
  • [18F]SynVesT-2 (SDM2)
Target
  • Synaptic vesicle 2A (SV2A)
Example Uses
  • Neuropsychiatric disorders
[11C]UCB-J
Synaptic vesicle 2A (SV2A)
Neuropsychiatric disorders
[18F]SynVesT-1 (SDM8)
Synaptic vesicle 2A (SV2A)
Neuropsychiatric disorders
[18F]SynVesT-2 (SDM2)
Synaptic vesicle 2A (SV2A)
Neuropsychiatric disorders

Channel like target

Tracer
  • [11C]PBR28
Target
  • Peripheral Benzodiazepine Receptor
Example Uses
  • Neuroinflammation
[11C]PBR28
Peripheral Benzodiazepine Receptor
Neuroinflammation

Aggregated protein target

Tracer
  • [11C]PIB
  • [18F]MK6240
  • [11C]M503
Target
  • Beta-Amyloid Plaques
  • Tau protein aggregates
  • α-synuclein
Example Uses
  • AD
  • PD
[11C]PIB
Beta-Amyloid Plaques
AD
[18F]MK6240
Tau protein aggregates
AD
[11C]M503
α-synuclein
PD

Cancer

Tracer
  • [11C]Erlotinib
  • [11C]PyBic
  • [18F]FMISO
  • [11C]Methionine
  • [18F]BMS-986192
  • [18F]BMS-986229
  • [64Cu]CuCl2
  • [89Zr]Df-crefmirlimab
Target
  • Epidermal Growth Factor Receptor (EGFR)
  • poly(ADP-ribose) polymerase (PARP) inhibitor
  • HIF1α
  • Protein Synthesis
  • Programmed cell death ligand (PDL1)
  • Copper uptake
  • CD8 T-cells
Example Uses
  • NSCLC
  • Oncology, neurodisease
  • Tumor hypoxia
  • Cancer
[11C]Erlotinib
Epidermal Growth Factor Receptor (EGFR)
NSCLC
[11C]PyBic
poly(ADP-ribose) polymerase (PARP) inhibitor
Oncology, neurodisease
[18F]FMISO
HIF1α
Tumor hypoxia
[11C]Methionine
Protein Synthesis
Cancer
[18F]BMS-986192
Programmed cell death ligand (PDL1)
Cancer
[18F]BMS-986229
Programmed cell death ligand (PDL1)
Cancer
[64Cu]CuCl2
Copper uptake
Cancer
[89Zr]Df-crefmirlimab
CD8 T-cells
Cancer

Others

Tracer
  • [F-18]PEG-biotin
  • [F-18]TPP
Target
  • Drug delivery (nanoparticle)
  • Myocardial mitochondrial
Example Uses
  • Tumors, CNS disease
  • Cardiac injury
[F-18]PEG-biotin
Drug delivery (nanoparticle)
Tumors, CNS disease
[F-18]TPP
Myocardial mitochondrial
Cardiac injury

Selected PET Radioligands

Dopamine D2/D3 receptor

Radiotracer: [11C]PHNO

Target: Dopamine D2/D3 receptor

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