NOP-1A

Biological Activity

NOP-1A standard. 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.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.