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Chlorprothixene Dopamine Receptor antagonist

Name: Chlorprothixene
Brand: Selleck Chemicals
SKU: S1771
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S1771

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 K_i of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

Chemical Structure

Molecular Weight: 315.86

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.42%

99.42

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR MAO Beta Amyloid iGluR NMDAR P2 Receptor Trk receptor Serotonin Transporter Notch Norepinephrine Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor CCK receptor
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Chemical Information, Storage & Stability

Molecular Weight	315.86	Formula	C₁₈H₁₈ClNS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	113-59-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Minithixen,Truxal			Smiles	CN(C)CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl

Solubility

In vitro
Batch:

Ethanol : 28 mg/mL

DMSO : 6 mg/mL (18.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	The first, typical antipsychotic drug of the thioxanthene class to be synthesized.
Targets/IC₅₀/Ki	D2 receptor ^[1] 2.96 nM(Ki) 5-HT6 ^[2] 3 nM(Ki) H1 receptor ^[1] 3.75 nM(Ki) D3 receptor ^[1] 4.56 nM(Ki) 5-HT7 ^[2] 5.6 nM(Ki) D5 receptor ^[1] 9 nM(Ki) 5-HT2 ^[2] 9.4 nM(Ki) D1 receptor ^[1] 18 nM(Ki)
In vitro	Chlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with K_i values of 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (K_i >1000 nM). ^[1] This compound 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 K_i values of 3 nM and 5.6 nM, respectively. ^[2] Administration of this chemical 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 this compound 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 this chemical 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/19091563/ [2] https://pubmed.ncbi.nlm.nih.gov/7908055/ [3] https://pubmed.ncbi.nlm.nih.gov/18423639/ [4] https://pubmed.ncbi.nlm.nih.gov/13704858/ [5] https://pubmed.ncbi.nlm.nih.gov/19635928/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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