| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H21ClN2O |
| Molecular Weight | 351.858 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC[C@@H](C)N([11CH3])C(=O)C1=NC(C2=CC=CC=C2Cl)=C3C=CC=CC3=C1
InChI
InChIKey=RAVIZVQZGXBOQO-NIQXDKTISA-N
InChI=1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3/t14-/m1/s1/i3-1
| Molecular Formula | C21H21ClN2O |
| Molecular Weight | 351.858 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
PK-11195 is a selective antagonist of the Translocator Protein (TSPO). The C11 radiolabeled isotope of PK-11195 ([11C]-(R)-PK-11195) has been used effectively for diagnostic PET imaging in a number of CNS conditions where imaging of TSPO is informative (the S- enantiomer is not used). Applicable conditions including Schizophrenia, Multiple Sclerosis, and Traumatic Brain Injuries where it has been particularly useful for detection of increased microglial activation. It has also been investigated as means to monitor the role of Toll-Like Receptor-4 (TLR-4) after cerebral ischemia in mice. It should be noted that the unlabeled PK-11195 had been investigated for a number of potential therapeutic uses but did not progress beyond animal and cell models.
CNS Activity
Approval Year
Doses
Sourcing
PubMed
Patents
Sample Use Guides
For PET imaging in glioma patients and healthy volunteers [11C]-(R)PK11195 was administered intravenously as a slow bolus over 15 seconds in a dose of 1.6 ± 0.8 micrograms and 2.4 ± 2.1 micrograms respectively. All PET scans were performed on a high-resolution research tomograph. Emission data were then acquired over 60 min in list mode as 18 time-frames
Route of Administration:
Intravenous
