Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H30N4O2S2 |
Molecular Weight | 446.629 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)S(=O)(=O)C1=CC2=C(SC3=CC=CC=C3N2CCCN4CCN(C)CC4)C=C1
InChI
InChIKey=VZYCZNZBPPHOFY-UHFFFAOYSA-N
InChI=1S/C22H30N4O2S2/c1-23(2)30(27,28)18-9-10-22-20(17-18)26(19-7-4-5-8-21(19)29-22)12-6-11-25-15-13-24(3)14-16-25/h4-5,7-10,17H,6,11-16H2,1-3H3
DescriptionSources: https://www.drugbank.ca/drugs/DB01622Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/thioproperazine.html | https://www.ncbi.nlm.nih.gov/pubmed/13661859 | https://www.ncbi.nlm.nih.gov/pubmed/16777448 | https://www.ncbi.nlm.nih.gov/pubmed/1354163 | https://www.ncbi.nlm.nih.gov/pubmed/4379824 | http://eci2012.net/wp-content/uploads/2015/03/Majeptil-PM-En-160702.01-20Feb2015.pdf
Sources: https://www.drugbank.ca/drugs/DB01622
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/thioproperazine.html | https://www.ncbi.nlm.nih.gov/pubmed/13661859 | https://www.ncbi.nlm.nih.gov/pubmed/16777448 | https://www.ncbi.nlm.nih.gov/pubmed/1354163 | https://www.ncbi.nlm.nih.gov/pubmed/4379824 | http://eci2012.net/wp-content/uploads/2015/03/Majeptil-PM-En-160702.01-20Feb2015.pdf
Thioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16777448 |
0.45 nM [Ki] | ||
Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1354163 |
1.2 nM [Ki] | ||
Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16288681 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Majeptil Approved UseINDICATIONS. All types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. |
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Primary | Majeptil Approved UseINDICATIONS. All types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. |
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Primary | Majeptil Approved UseINDICATIONS. All types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. |
Sample Use Guides
Adults: It is recommended to start treatment at a low dosage of about 5 mg per day in a single dose or in divided doses. This initial dosage is gradually increased by the same amount every 2 to 3 days until the usual effective dosage of 30 to 40 mg per day is reached. In some cases higher dosages of 90 mg or more per day, are necessary to control the psychotic manifestations. Children: In children over 10 years: Start treatment with a daily dosage of 1 to 3 mg following the method of treatment described for adults.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3926530
The effects of drugs on biochemical parameters of red blood cells were assessed using 100 ml human blood, which was obtained from a volunteer and diluted with 15 ml of 16 mM citric acid, 113 mM sodium citrate, 21 mM monosodium phosphate, 140 mM glucose, and 2 mM adenine at pH 7.4. Thioproperazine samples were added to 10-ml aliquots of blood to give a final concentration of 1 mM, and the blood was stored at 4 C. The pH of the blood was routinely measured, and 2-ml samples were taken. The cells were pelleted by centrifugation at 3000gma x for 5 rain, and the supernatants were removed. Two volumes of 15% (w/v) trichloroacetic acid were added to 1 vol of packed cells and, after standing on ice for 10 rain, the denatured protein was removed by centrifugation. The acid-soluble fraction was extracted four times with copious amounts of water-saturated diethyl ether to remove the trichloracetic acid and was assayed for 2,3-diphosphoglyceric acid levels using spectrophotometric methods
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WHO-VATC |
QN05AB08
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NCI_THESAURUS |
C29710
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WHO-ATC |
N05AB08
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SUB10983MIG
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59120
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2635
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100000082127
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10498
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911
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9429
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m10780
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316-81-4
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DB01622
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YJ050AQ56X
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DTXSID1023655
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C084825
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206-262-4
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C73292
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THIOPROPERAZINE
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CHEMBL609109
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)