Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 492-27-3, is researched, Molecular C10H7NO3, about Phase 1 study to access safety, tolerability, pharmacokinetics, and pharmacodynamics of kynurenine in healthy volunteers, the main research direction is human nervous system kynurenine safety tolerability pharmacokinetics pharmacodynamics; epilepsy; glutamat; kynurenic acid; migraine; stroke.COA of Formula: C10H7NO3.
The kynurenine pathway (KP) is the main path for tryptophan metabolism, and it represents a multitude of potential sites for drug discovery in neuroscience, including pain, stroke, and epilepsy. L-kynurenine (LKYN), the first active metabolite in the pathway, emerges to be a prodrug targeting glutamate receptors. The safety, tolerability, pharmacokinetics, and pharmacodynamics of LKYN in humans have not been previously investigated. In an open-label, single ascending dose study, six participants received an i.v. infusion of 50, 100, and 150μg/kg LKYN and new six participants received an i.v. infusion of 0.3, 0.5, 1, and 5 mg/kg LKYN. To compare the pharmacol. effects between species, we investigated in vivo the vascular effects of LKYN in rats. In humans, LKYN was safe and well-tolerated at all dose levels examined After infusion, LKYN plasma concentration increased significantly over time 3.23 ± 1.12μg/mL (after 50μg/kg), 4.04 ± 1.1μg/mL (after 100μg/kg), and 5.25 ± 1.01μg/mL (after 150μg/kg) (p < 0.001). We observed no vascular changes after infusion compared with baseline. In rats, LKYN had no effect on HR and MAP and caused no dilation of dural and pial arteries. This first-in-human study of LKYN showed that LKYN was safe and well-tolerated after i.v. infusion up to 5 mg/kg over 20 min. The lack of change in LKYN metabolites in plasma suggests a relatively slow metabolism of LKYN and no or little feed-back effect of LKYN on its synthesis. The therapeutic potential of LKYN in stroke and epilepsy should be explored in future studies in humans. There are many compounds similar to this compound(492-27-3)COA of Formula: C10H7NO3. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.
Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”