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Penfluridol Dopamine Receptor antagonist

Cat.No.S4151

Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Penfluridol Dopamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 523.97

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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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.
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Chemical Information, Storage & Stability

Molecular Weight 523.97 Formula

C28H27ClF5NO

Storage (From the date of receipt)
CAS No. 26864-56-2 Download SDF Storage of Stock Solutions

Synonyms TLP-607,R-16341 Smiles C1CN(CCC1(C2=CC(=C(C=C2)Cl)C(F)(F)F)O)CCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F

Mechanism of Action

Targets/IC50/Ki
Dopamine receptor
(Cell-free assay)
1.6 μM(Ki)
In vitro

Penfluridol is a neuroleptic drug with long duration of action, which is able to relieve both negative and positive symptoms of schizophrenia. It inhibits the binding of dopamine to dopamine receptor with Ki of 1.6 μM. This compound exerts its antipsychotic activity by blocking the dopamine projections in the limbic system and in mesocortical area. The chemical selectively inhibits the binding of [3H]nitrendipine to rat cerebral cortical membrane fraction and also competitively antagonizes potassium-induced calcium-dependent contractions in rat vas deferens. This agent (10 μM) inhibits the contractile response of isolated rings of rabbit thoracic aorta to NE and KCl, and inhibits calcium influx during either NE or KCl stimulation.

References

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