Chlorprothixene

製品コードS1771 バッチS177101

印刷

化学情報

Chemical Structure Synonyms Minithixen,Truxal Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H18ClNS
分子量 315.86 CAS No. 113-59-7
Solubility (25°C)* 体外 Ethanol 28 mg/mL (88.64 mM)
DMSO 6 mg/mL (18.99 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
in vitro

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 μM for Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1 and 15.8 μM for Toronto-2. There are similar to those detected with promazine [3]
in vivo

Chlorprothixene blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain depressing the release of hypothalamic and hypophyseal hormones. High dose of chlorprothixene inhibits the protection afforded by iproniazid against the reserpine-induced release of catecholamines in adrenal medulla and brain as well as the decrease of 5HT, NE and DA due to reserpine or iproniazid in rat brain. [4] Administration of Chlorprothixene restores normal ceramide concentrations in murine bronchial epithelial cells, reduces inflammation in the lungs of mice with cystic fibrosis (CF) and prevents infection with Pseudomonas aeruginosa, by inhibiting acidsphingomyelinase (Asm) and not neutral sphingomyelinase (Nsm). [5]
特徴 The first, typical antipsychotic drug of the thioxanthene class to be synthesized.

プロトコル(参考用のみ)

キナーゼアッセイ 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 μM clozapine and represented at least 95% of total binding. Competition and saturation binding data are analyzed by using the LIGAND program.
動物実験 動物モデル B6.129P2 (CF/3)-CftrTgH(neoim)Hgu (abbreviated CFMHH) congenic mice.
投薬量 1 mL every time
投与方法 Five 10-minute inhalations, every 12 hours

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904] PubMed: 36386620
Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. [ Sci Rep, 2018, 8(1):15753] PubMed: 30361678

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。