| [11C]A1070722 |
to identify a brain-penetrating GSK3 radioligand |
1H NMR |
- in vivo primate
PET scan |
(56) |
| HRMS |
- 11C-metabolite study with HPLC fractions |
| HPLC-UV |
|
| [11C]AZ683 |
AZ683 has a high and selective affinity for Colony
Stimulating Factor 1 Receptor (CSF1R). |
1H
NMR |
- in vivo primate and rodent PET
scan |
(27) |
| HRMS |
|
| HPLC-UV |
|
| [11C]CMP |
11C-structural analogue
of a high affinity
Glycogen synthase kinase 3 (GSK3) ligand |
1H NMR |
- in vitro cell uptake assay |
(57) |
| HRMS |
- in vivo rodent microPET |
| HPLC-UV |
|
| [11C]CPPC |
CPPC
was demonstrated to have high affinity and
specificity for CSF1R. |
1H NMR |
- in vivo primate and rodent PET scan39
|
(39,40) |
| HRMS |
- in vitro cell binding assays |
| HPLC-UV |
- later clinical
study40
|
| [11C]dLop |
Identified as a metabolite of [11C]loperamide
that showed higher affinity for P-Glycoprotein (P-gp) |
1H NMR |
- In vivo primate
and rodent PET scan |
(58,59) |
|
13C NMR |
- 11C-metabolite study
with HPLC fractions |
| LC-MS/MS |
- clinical study58
|
| HPLC-UV |
|
| [11C]6,7-dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline |
Computer assisted drug design (CADD) docking studies
were performed on 46 known to have high σ2 receptor affinity
and the most promising compound was selected. |
1H NMR |
- in vitro cell binding assays |
(60) |
|
13C NMR |
- distribution coefficient log D7.4
|
| LC-MS (ESI) |
determined |
| HRMS |
- ex vivo tissue binding study |
| |
- in vivo rodent
PET scan |
| |
- 11C metabolite study with HPLC fractions |
| [11C]GSK1838705A |
GSK1838705A is a high affinity and selective ligand
for IGF1R/IR kinase. |
1H NMR |
- in vivo rodent microPET/CT |
(61) |
| HRMS |
- in
vitro study with human cells |
| HPLC-UV |
|
| [11C]GSK2126458 |
GSK2126458 is a known PI3K and mTOR kinase inhibitor. |
1H NMR |
- not assessed in this study |
(62) |
| HPLC-UV |
|
| [11C]HC070 |
similar chemical structures to existing radiotracers
that target TRPC5 |
HRMS |
- in vitro
|
(26) |
|
1H
NMR |
- in vivo rodent and primate PET
scan |
|
13C NMR |
- ex vivo biodistribution studies |
| [11C]HD-800 |
HD-800 is known to be an inhibitor with high affinity
and selectivity of the target colchicine site of microtubules. |
1H NMR |
- ex vivo biodistribution
studies |
(63) |
| HRMS |
- in vivo rodent PET scan |
| HPLC-UV |
|
| [11C]KSM-01 |
similar chemical structure to a known selective
and high affinity ligand to the PPAR-α target protein complex |
1H NMR |
- in vivo rodent
microPET |
(64) |
|
13C NMR |
- in vitro binding study |
| HPLC-UV |
|
| melting point |
|
| [11C]LAAM |
clinically used to prevent opioid withdrawal |
HPLC-UV |
- in vivo rodent microPET |
(65) |
| |
- ex vivo biodistribution |
| [11C]LY2459989 |
The authors wanted to develop a more selective
radiotracer for κ-opioid receptors. |
1H NMR |
- in vivo primate PET scan |
(66) |
| HPLC-MS |
- in vitro binding assays |
| chiral HPLC-UV |
- ex vivo biodistribution
rodent studies |
| [11C]LY2795050 |
known antagonist
κ-opioid receptors |
1H NMR |
- in vitro binding study44
|
(43,44,67) |
| HPLC-UV |
- ex vivo biodistribution44
|
| |
- in vivo primate study44
|
| |
- later clinical study43,67
|
| [11C]MPC-6827 |
MPC-6827 has high affinity and selectivity for
microtubules. |
1H NMR |
- lipophilicity
determination |
(35,68) |
| LC-MS/MS |
- ex vivo biodistribution |
| HPLC-UV |
- in vivo rodent microPET/CT |
| |
- in vivo primate study68
|
| [11C]OCM-44 |
GSK3
inhibitor with high affinity and selectivity.
It also has a similar chemical structure to previously reported radiotracers. |
1H NMR |
- in vivo primate
PET69
|
(69,70) |
|
13C NMR |
- metabolite analysis
with HPLC69
|
| - blocking studies69
|
| HRMS |
- in silico docking study70
|
| HPLC-UV |
| [11C]ORM-13070 |
A radiotracer specific to the α2c adrenoceptor was developed. |
HPLC-UV |
- in vivo rodent PET/CT |
(49,71) |
| - ex vivo binding specificity
assessment |
| - clinical PET71
|
| [11C]ORM-13070- like radiotracers |
similar chemical structures to [11C]ORM-13070,identified
with CADD docking studies to potentially increase selectivity for
the α2c adrenoceptor |
1H NMR |
-radiochemical stability |
(48) |
| - in vitro cell
binding assay |
|
13C NMR |
- ex vivo biodistribution studies |
| LC-MS (ESI) |
- in vivo rat studies |
| N-[11C]meisoindigotin |
11C-methylated
structural analogue of cancer chemotherapeutic
agent |
LC-MS/MS |
- in vitro lung cancer cell lines |
(54) |
| [11C]PyrATP-1 |
high
affinity and selectivity for the ATP binding
site |
1H NMR |
- in vivo primate and rodent microPET |
(72) |
|
13C NMR |
- ex vivo rat brain studies |
| HRMS |
| HPLC-UV |
| [11C]RO6931643 and [11C]RO6924963 |
Both compounds were identified as high-affinity
competitors to the target tau aggregate binding site in Alzheimer’s
disease. |
HPLC-UV |
- in vivo primate studies73
|
(73,74) |
|
1H NMR |
- ex vivo human brain tissue studies73
|
| LC-HRMS |
- passive membrane permeability (PAMPA)74
|
| - determination
of affinity74
|
| - lipophilicity (log D)74
|
| - brain lipid
membrane binding (LIMBA log Dbrain)74
|
| [11C]UCB-J |
UCB-J
was identified to be a high affinity ligand
to Synaptic Vesicle Glycoprotein 2A in the brain. |
1H NMR |
- in vivo primate and
rodent PET |
(53,75,76) |
| HRMS |
- in vitro cell binding assay |
| - lipophilicity (log D7.4) determined |
| chiral HPLC-UV |
- metabolite analysis with gamma-counter |
|
| - clinical
studies75
|
| [11C]VAChT ligand |
Twenty new compounds were synthesized and evaluated in vitro, and the compound with the strongest binding affinity
for the vesicular acetylcholine transporter (VAChT) was radiolabeled. |
X-ray crystallography |
- in vitro binding affinities where assayed |
(77) |
| - lipophilicity (log D7.4) determined |
| - in vivo rat and primate studies |
| - ex vivo biodistribution |
|
1H NMR |
|
| [11C]WX-132–18B |
high-affinity agent for the targeted microtubules |
1H NMR |
- in vivo rodent microPET/CT |
(78) |
| HRMS |
| HPLC-UV |
| melting point |
