Chlorprothixene

Catalog No.S1771

For research use only.

Chlorprothixene 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.

Chlorprothixene Chemical Structure

CAS No. 113-59-7

Selleck's Chlorprothixene has been cited by 1 Publication

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Biological Activity

Description Chlorprothixene 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.
Features The first, typical antipsychotic drug of the thioxanthene class to be synthesized.
Targets
D2 receptor [1] 5-HT6 [2] H1 receptor [1] D3 receptor [1] 5-HT7 [2] Click to View More Targets
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]

Protocol (from reference)

Animal Research:[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

Solubility (25°C)

In vitro

Ethanol 28 mg/mL
(88.64 mM)
DMSO 6 mg/mL
(18.99 mM)
Water Insoluble

Chemical Information

Molecular Weight 315.86
Formula

C18H18ClNS

CAS No. 113-59-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03449485 Recruiting Drug: Chlorprothixene Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital January 2 2018 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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