Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H23F4NO2.ClH |
Molecular Weight | 445.878 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)C3=CC=CC(=C3)C(F)(F)F
InChI
InChIKey=VYGQXRZAHIZHQV-UHFFFAOYSA-N
InChI=1S/C22H23F4NO2.ClH/c23-19-8-6-16(7-9-19)20(28)5-2-12-27-13-10-21(29,11-14-27)17-3-1-4-18(15-17)22(24,25)26;/h1,3-4,6-9,15,29H,2,5,10-14H2;1H
Trifluperidol is an antipsychotic butyrophenone derivative. It is a high-affinity sigma receptor blocker and it was strongly selective for NR1a/2B receptors. It exhibit pharmacological effects and a mechanism of action very similar to that of phenothiazines and thioxanthenes in that it blocks dopaminergic receptors. It is more selective with respect to D2 receptors. Trifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. Trifluperidol has been suspected as a cause of cataract in Japan. Patients receiving trifluperidol treatment may develop a parkinsonian-like syndrome which responds to withdrawal of the drug or concurrent administration of an anti-parkinsonian drug. Acute dystonias and akathisia are other acute extrapyramidal effects; tardive dyskinesia may supervene after longer periods of treatment.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL217 Sources: DOI: 10.1021/om901011t |
|||
Target ID: CHEMBL3602 |
0.83 nM [Ki] | ||
Target ID: CHEMBL2096666 |
1.2 µM [IC50] | ||
Target ID: CHEMBL2096680 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9223571 |
69.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Triperidol Approved UseTrifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. |
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Primary | Triperidol Approved UseTrifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. |
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Primary | Triperidol Approved UseTrifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. |
Sample Use Guides
Initial dose - 0.5 mg daily, increased at intervals of 3-4 days until improvement occurs or a total dose of 6-8 mg daily is reached.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15591644
The effect of neuroleptics on the release of proinflammatory cytokines (IL-1beta and IL-2) by mixed glial and microglial cell cultures was investigated. Trifluperidol at 20 and 2 uM reduced IL-beta secretion by mixed glial cultures after 3 days of exposure. Trifluperidol at 20, 2 and 0.2 uM diminished IL-beta secretion after 1 day of incubation. Trifluperidol at 20 and 2 uM reduced IL-2 release after 1 and 3 days of exposure.
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218-170-1
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16361
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236140
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SUB04957MIG
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2062-77-3
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100000084663
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169875
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m11122
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UIC8RB6P81
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DTXSID2045810
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ACTIVE MOIETY
SUBSTANCE RECORD