Chlorprothixene

2 years -80 in solvent

Five 10-minute inhalations, every 12 hours

Under clinical trails for studying the prevention of relapse in Schizophrenia.

Dissolved in 0.9% NaCl solution, final concentration 8 mg/L

Chlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with Ki values of 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (Ki >1000 nM). [1] Chlorprothixene also shows high affinities for both rat 5-HT6 from stably transfected HEK-293 cells, and rat 5-HT7 receptors from transiently expressed COS-7 cells, with Ki values of 3 nM and 5.6 nM, respectively. [2] Administration of chlorprothixene results in inhibition of SARS-CoV replication in Vero 76 cells, with IC50 of 16.7 uM for Urbani strain, 13.0 uM for Frankfurt-1, 18.5 uM for CHUK-W1 and 15.8 uM for Toronto-2. There are similar to those detected with promazine [3]

[2], Radioligand binding assay, COS-7 cells transfected with p5HT7 or pSVK3-5HT1C and HEK-293 cells that express the 5-HT6 receptor are washed with PBS twice for 10 minutes each and then harvested with a cell scraper into 20 mL PBS. After concentration by centrifugation, cells are lysed in binding buffer (50 mM Tris-HCl, pH 7.4) and membranes are collected by centrifugation. [3H]-LSD binding assays for 5-HT6 and 5-HT7 are performed in a total volume of 0.2 or 0.5 mL, respectively, at 25 C for 90 minutes in the dark. After incubation, the membranes are collected onto polyethyleneimine-pretreated glass fiber filters, washed with 5 mL of ice-cold binding buffer three times and then quantified by liquid scintillation spectrophotometry. Quenching is corrected by the sample channels ratio technique. Nonspecific binding is determined with 10 uM clozapine and represented at least 95% of total binding. Competition and saturation binding data are analyzed by using the LIGAND program.

Chlorprothixene(Minithixen, Truxal) has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.