We studied the brain uptake of a new 2-amino-2-oxazolamines derivative (COR3224) in the rat by means of the rapid intracarotid injection technique described by Oldendorf. The brain uptake index (BUI) of labelled COR3224 decreased progressively from 10% to 5% when concentrations of unlabelled compound were increased. The effect of various compounds indicated that COR3224 is transported into the brain by the purine carrier. The affinity of COR3224 for this carrier (Km = 5.68 microM) was higher than that of adenine.

01 Feb 1991·Journal of Chromatography B: Biomedical Sciences and Applications

Determination of a new 2-amino-2-oxazoline (COR 3224) in plasma and brain tissue of the rat by high-performance liquid chromatography with electrochemical detection

Article

Author: C. Jacquot ; J.H. Trouvin ; M.I. Damaj ; B. Lambrey

A reversed-phase (CN as stationary phase) liquid chromatographic method with electrochemical detection is described for the quantitation of COR 3224, a new 2-amino-2-oxazoline in plasma and brain tissue of the rat. Extraction was performed with dichloromethane and detection was achieved at a working electrode potential of +0.85 V versus an Ag/AgCl reference electrode. The recovery of the method is about 80 and 60% for plasma and brain, respectively. The limit of detection was less than 10 ng/ml for both plasma and brain, five times lower than that with ultraviolet detection.

01 Jan 1991·European journal of drug metabolism and pharmacokineticsQ4 · MEDICINE

Kinetics and brain uptake of COR3224, a new 2-amino-2-oxazoline, in rats.

Q4 · MEDICINE

Article

Author: Trouvin, J H ; Lambrey, B ; Damaj, M I ; Jacquot, C

COR3224, a new 2-amino2 oxazoline derivative, shows antidepressant activity in the rat. This study was designed to analyse the influence of dose ranging on the brain/plasma concentration ratio of this drug. Adult male rats (250-300gr, Sprague Dawley) were given orally 10, 40 and 160 mg/Kg radiolabelled 14C-COR3224 (30 microCi/kg) in aqueous solution and were sacrificed at 0.25; 0.5; 0.75; 1; 2; 4; 6; 8; 12; 16; 24; and 30 hours post dose (5 rats per time). Plasma and brain samples were analysed for total radioactivity (T.R.) by liquid scintillation and for COR3224 (U.P.) by reversed-phase liquid chromatography and electrochemical detection. A linear relationship was found between AUC and doses administered for both TR and UP plasmatic determinations. In opposite, cerebral AUC for TR and U.P were not proportional to dose, and the evolution of the brain/plasma concentration ratios showed higher values for the 10mg/kg dose than for the 40 and 160mg/kg doses.

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Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder	Phase 2	-	Arisyn Therapeutics Inc	-
Depressive Disorder, Major	Phase 2	DE	ASTA Medica AG	-

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