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Details

Stereochemistry ACHIRAL
Molecular Formula C22H24FN3OS
Molecular Weight 397.509
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TIMIPERONE

SMILES

FC1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)N3C(=S)NC4=C3C=CC=C4

InChI

InChIKey=YDLQKLWVKKFPII-UHFFFAOYSA-N
InChI=1S/C22H24FN3OS/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28/h1-2,4-5,7-10,18H,3,6,11-15H2,(H,24,28)

HIDE SMILES / InChI

Description

Timiperone is a neuroleptic agent that was developed in Japan. Timiperone has a potent antipsychotic activity, which is comparable to other butyrophenones such as haloperidol (HAL). Timiperone has a five-eight-times higher affinity to dopamine receptors and a 15-times higher affinity to serotonin receptors than those of HAL. Clinical trials have suggested that TIM has a specific action against negative symptoms such as lack of initiative or blunted affect as well as positive symptoms such as delusions and hallucinations in schizophrenics.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Tolopelon

Cmax

ValueDoseCo-administeredAnalytePopulation
5.947 ng/mL
6 mg single, oral
TIMIPERONE plasma
Homo sapiens
13.6 ng/mL
4 mg single, intramuscular
TIMIPERONE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
39.321 ng × h/mL
6 mg single, oral
TIMIPERONE plasma
Homo sapiens
175.3 ng × h/mL
4 mg single, intramuscular
TIMIPERONE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
5.906 h
6 mg single, oral
TIMIPERONE plasma
Homo sapiens
15.7 h
4 mg single, intramuscular
TIMIPERONE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
TIMIPERONE plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
Dosage gradually increase from 0,5-3 mg to 3-12 mg daily during 12 weeks
Route of Administration: Other
In Vitro Use Guide
Unknown