The International Journal of Applied Radiation and Isotopes
Radiosynthesis of an opiate receptor binding radiotracer: [11C]carfentanil
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Cited by (140)
Tactics for preclinical validation of receptor-binding radiotracers
2017, Nuclear Medicine and BiologyCitation Excerpt :So, if detailed in vitro binding studies are needed, tritium-labeled ligands (t1/2 12.3 y; 6 keV, β−) with specific activities of 29 Ci/mmol or higher, depending on level of tritium incorporation, are used. A notable example is [3H]-carfentanil characterization of in vitro binding in human brain tissue to aid interpretation of PET studies of μ opioid receptors using [11C]-carfentanil [60–62]. With this backdrop, a more detailed description of the radiopharmaceutical paradigm is shown in Chart 2, where a variety of experiments are listed that help define receptor-binding radiotracers.
Buprenorphine maintenance and mu-opioid receptor availability in the treatment of opioid use disorder: Implications for clinical use and policy
2014, Drug and Alcohol DependenceCitation Excerpt :If we assume that μOR affinity and endogenous ligand concentrations are constant, then a reduction in μOR availability is proportional to an increase in “occupancy.” In studies reported here, [11C]-carfentanil was synthesized to have μOR-specific activity (Dannals et al., 1985; Jewett, 2001), and administered IV in a small mass (≈ 0.03 μg/kg per scan) to ensure only sub-pharmacological amounts that occupy 0.3–0.6% of μORs. Half the total dose was administered as a bolus and the remainder as a continuous infusion, calibrated to offset [11C]-carfentanil elimination rate.
Evaluation of the agonist PET radioligand [<sup>11</sup>C]GR103545 to image kappa opioid receptor in humans: Kinetic model selection, test-retest reproducibility and receptor occupancy by the antagonist PF-04455242
2014, NeuroImageCitation Excerpt :As such, KOR is a target for development of newer antidepressants. There have been no prior reports of validated PET radiotracers for use in humans to image the KOR, although several tracers have been proposed and validated for MOR (Dannals et al., 1985), for MOR and KOR (Pert et al., 1984), and for DOR (Kinter and Lever, 1995). GR89696 ((±)-4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazine carboxylate) is a potent KOR agonist (Naylor et al., 1993).
The Synthesis of Biphasic Metabolites of Carfentanil
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