Drug intelligence / Profile preview

[18F]1a

Development stage
Preclinical
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]1a is an experimental radiopharmaceutical and small molecule radiotracer designed for positron emission tomography (PET) imaging of opioid receptors. Chemically, it is an N-fluoroalkyl analogue of diprenorphine, a potent and non-selective opioid receptor antagonist. Labeled with the positron-emitting radionuclide fluorine-18, [18F]1a enables the non-invasive visualization and quantification of opioid receptor distribution and binding kinetics in the central nervous system. The compound is synthesized via a two-step radiolabeling procedure involving fluoride displacement followed by N-alkylation, typically resulting in a radiochemical yield of 0.3-0.6%. It has been primarily utilized in preclinical research to study receptor density and ligand-receptor interactions in vivo.

Other names
N-([18F]fluoroalkyl)diprenorphine[18F]fluoroalkyldiprenorphine
02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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