Rover, Stephan published the artcile6-Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds, Formula: C6H4BrNO3, the main research area is alkoxy arylpyridinecarboxamide preparation bioavailable cannabinoid CB1 antagonist.
The authors identified 6-alkoxy-5-aryl-3-pyridinecarboxamides as potent CB1 receptor antagonists with high selectivity over CB2 receptors. The series was optimized to reduce lipophilicity compared to rimonabant to achieve peripherally active mols. with minimal central effects. Several compounds that showed high plasma exposures in rats were evaluated in vivo to probe the contribution of central vs peripheral CB1 agonism to metabolic improvement. Both rimonabant and I, a potent brain penetrant CB1 receptor antagonist, significantly reduced the rate of body weight gain. However, II, a mol. with markedly reduced brain exposure, had no significant effect on body weight PK studies confirmed similarly high exposure of both I and II in the periphery but 10-fold lower exposure in the brain for II. On the basis of these data, which are consistent with reported effects in tissue-specific CB1 receptor KO mice, it was concluded that the metabolic benefits of CB1 receptor antagonists are primarily centrally mediated as originally believed.
Journal of Medicinal Chemistry published new progress about Antiobesity agents. 41668-13-7 belongs to class bromides-buliding-blocks, name is 5-Bromo-6-hydroxynicotinic acid, and the molecular formula is C6H4BrNO3, Formula: C6H4BrNO3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary