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- Title
Synthesis of <sup>13</sup>C<sub>6</sub>‐labeled, dual‐target inhibitor of cannabinoid‐1 receptor (CB<sub>1</sub>R) and inducible nitric oxide synthase (iNOS).
- Authors
Iyer, Malliga R.; Cinar, Resat; Coffey, Nathan J.; Kunos, George
- Abstract
Cannabinoid‐1 receptor (CB1R) antagonists/inverse agonists have great potential in the treatment of metabolic disorders like dyslipidemia, type 2 diabetes, and nonalcoholic steatohepatitis. Cannabinoid‐1 receptor inverse agonists have also been reported to be effective in mitigating fibrotic disorders in murine models. Inducible nitric oxide synthase is another promising target implicated in fibrotic and inflammatory disorders. We have disclosed MRI‐1867 as a potent and selective, peripherally acting dual‐target inhibitor of the CB1R and inducible nitric oxide synthase (iNOS). Herein, we report the synthesis of [13C6]‐MRI‐1867 as a racemate from commercially available chlorobenzene‐13C6 as the starting, stable‐isotope label reagent. The racemic [13C6]‐MRI‐1867 was further processed to the stable‐isotope‐labeled enantiopure compounds using chiral chromatography. Both racemic [13C6]‐MRI‐1867 and S‐13C6‐MRI‐1867 will be used to quantitate unlabeled S‐MRI‐1867 during clinical drug metabolism and pharmacokinetics studies and will be used as a liquid chromatography‐tandem mass spectrometry bioanalytical standard.
- Subjects
CANNABINOID receptors; NITRIC-oxide synthases; DYSLIPIDEMIA; INFLAMMATION; CHLOROBENZENE; THERAPEUTICS
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2018, Vol 61, Issue 10, p773
- ISSN
0362-4803
- Publication type
Academic Journal
- DOI
10.1002/jlcr.3639