Chlorprothixene

Catalog No.S1771 Batch:S177101

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Technical Data

Formula

C18H18ClNS

Molecular Weight 315.86 CAS No. 113-59-7
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
D2 receptor [1] 5-HT6 [2] H1 receptor [1] D3 receptor [1] 5-HT7 [2] View More
2.96 nM(Ki) 3 nM(Ki) 3.75 nM(Ki) 4.56 nM(Ki) 5.6 nM(Ki)
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]

Features The first, typical antipsychotic drug of the thioxanthene class to be synthesized.

Protocol (from reference)

Animal Study:

[5]

  • Animal Models

    B6.129P2 (CF/3)-CftrTgH(neoim)Hgu (abbreviated CFMHH) congenic mice.

  • Dosages

    1 mL every time

  • Administration

    Five 10-minute inhalations, every 12 hours

Selleck's Chlorprothixene has been cited by 2 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.