Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H26F2N2O2S |
| Molecular Weight | 420.516 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC(=O)[C@H](CN1CCC2(CC1)OCCC3=C2SC(F)=C3)CC4=CC=CC=C4F
InChI
InChIKey=MZBCQWLYUQJXKA-KRWDZBQOSA-N
InChI=1S/C22H26F2N2O2S/c1-25-21(27)17(12-15-4-2-3-5-18(15)23)14-26-9-7-22(8-10-26)20-16(6-11-28-22)13-19(24)29-20/h2-5,13,17H,6-12,14H2,1H3,(H,25,27)/t17-/m0/s1
11C-NOP-1A is a new radioligand for thenociceptin/orphanin FQ peptide (NOP) receptor, with high affinity (Ki, 0.15 nM) and appropriate lipophilicity (measured logD, 3.4) for PET brain imaging. 11C-NOP-1A is the the first successful radioligand to image NOP receptors in rat and monkey brain. 11C-NOP-1A is a selective antagonist at the NOP receptor and has high affinity and appropriate lipophilicity for blood–brain barrier permeability. 11C-NOP-1A imaging in rhesus monkeys showed high brain uptake and a large receptor-specific signal and could be quantified with the gold standard method of compartmental modeling. In humans 1C-NOP-1A reliably quantified NOP receptors in human brain both in large brain regions and at a voxelwise level using parametric imaging. The radiation absorbed dose in humans was similar to that observed with other 11C-labeled ligands and would allow multiple scans of a single subject. Thus, 11C-NOP-1A is a promising radioligand for reliably quantifying NOP receptors in human brain.
Approval Year
Sample Use Guides
After intravenous injection of 11C-NOP-1A, 7 healthy subjects underwent brain PET for 2 h and serial sampling of radial arterial blood to measure parent radioligand concentrations. The radioligand was obtained with high radiochemical purity (>99%) and aspecific activity of 213 ± 100 GBq/umol at the time of injection. The injected mass dose of 11C-NOP-1A was 53 ± 36 pmol/kg. The effective dose of 11C-NOP-1A (4.3 uSv/MBq) estimated from whole-body scans inhumans was similar to previous estimates (5 uSv/MBq) from monkey studies and tothose of 34 other 11C-radioligands used for brain imaging, which ranged from 3 to 16 uSv/MBq.
Route of Administration:
Intravenous
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
52951810
Created by
admin on Sat Dec 16 08:06:29 GMT 2023 , Edited by admin on Sat Dec 16 08:06:29 GMT 2023
|
PRIMARY | |||
|
DB15208
Created by
admin on Sat Dec 16 08:06:29 GMT 2023 , Edited by admin on Sat Dec 16 08:06:29 GMT 2023
|
PRIMARY | |||
|
DQY244459T
Created by
admin on Sat Dec 16 08:06:29 GMT 2023 , Edited by admin on Sat Dec 16 08:06:29 GMT 2023
|
PRIMARY | |||
|
1283095-70-4
Created by
admin on Sat Dec 16 08:06:29 GMT 2023 , Edited by admin on Sat Dec 16 08:06:29 GMT 2023
|
PRIMARY |
SUBSTANCE RECORD
