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Fluoxetine HCl 5-HT Receptor Inhibitor

Kat.-Nr.S1333

Fluoxetine HCl ist ein selektiver Serotonin-Wiederaufnahmehemmer (SSRI) an der neuronalen Membran, der zur Behandlung von Depressionen eingesetzt wird.
Fluoxetine HCl 5-HT Receptor Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 345.79

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Qualitätskontrolle

Charge: Reinheit: 99.94%
99.94

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
HEK293 Function assay 30 mins Inhibition of human SERT expressed in HEK293 cells assessed as inhibition of serotonin reuptake after 30 mins by fluorescence assay, IC50=0.15μM 22938049
HEK293 Function assay 30 mins Inhibition of human NET expressed in HEK293 cells assessed as inhibition of noradrenaline reuptake after 30 mins by fluorescence assay, IC50=4.41μM 22938049
HEK293 Function assay 30 mins Inhibition of human DAT expressed in HEK293 cells assessed as inhibition of dopamine reuptake after 30 mins by fluorescence assay, IC50=18.4μM 22938049
mammalian cells Function assay Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=1.51356μM 12873512
JAR Function assay Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells, IC50=0.0324μM 15239661
K562 Cytotoxicity assay Cytotoxicity to reduce chronic myeloid leukemia K 562 cells, CC50=25μM 15267229
U937 Cytotoxicity assay Cytotoxicity to reduce human histolytic lymphoma U937 cells, CC50=33.3μM 15267229
HEK293 Function assay Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells, IC50=0.016μM 16750359
HEK293 Function assay Inhibition of DA transporter expressed in HEK293 cells, IC50=4.4μM 16750359
HEK293 Function assay Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells, IC50=5.2μM 16750359
HEK293 Function assay Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells, IC50=0.016μM 16750363
HEK293 Function assay Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells, IC50=4.4μM 16750363
HEK293 Function assay Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells, IC50=5.2μM 16750363
Jar Function assay Inhibition of [3H]5-HT uptake at human 5-HT transporter expressed in Jar cells, IC50=0.0394μM 16854086
SK-N-MC Function assay Displacement of N-[3H]alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells, Ki=7.3μM 17307358
CHO Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=1.51356μM 18448342
HEK293 Function assay Inhibition of serotonin uptake at human SERT in human HEK293 cells, IC50=0.047μM 18550369
HEK293 Function assay Inhibition of norepinephrine uptake at human NET in human HEK293 cells, IC50=2μM 18550369
HEK293 Function assay Inhibition of dopamine uptake at human DAT in human HEK293 cells, IC50=6μM 18550369
JAR Function assay Inhibition of 5HT uptake at human SERT expressed in human JAR cells, IC50=0.0094μM 18557608
HEK Function assay Inhibition of serotonin uptake at human SERT expressed in HEK cells, IC50=0.047μM 18667309
HEK Function assay Inhibition of norepinephrine uptake at human NET expressed in HEK cells, IC50=2μM 18667309
HEK Function assay Inhibition of dopamine uptake at human DAT expressed in HEK cells, IC50=6μM 18667309
JAR Function assay Inhibition of serotonin uptake at human SERT expressed in JAR cells, IC50=0.01μM 18771916
MDCK Function assay Inhibition of norepinephrine uptake at human NET expressed in MDCK cells, IC50=0.563μM 18771916
Jar Function assay Inhibition of 5-HT transporter-mediated [3H]5HT uptake in human Jar cells, IC50=0.0394μM 18834188
JAR Function assay Inhibition of serotonin uptake at human SERT expressed in JAR cells, IC50=0.0094μM 18951020
HEK293 Function assay Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells, Ki=0.0011μM 19014888
HEK293 Function assay Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells, IC50=0.007μM 19014888
HEK293 Function assay Inhibition of [3H]NE from human recombinant NET expressed in HEK293 cells, IC50=1.02μM 19014888
HEK293 Function assay Displacement of [125I]RTI55 from human recombinant NET expressed in HEK293 cells, Ki=1.56μM 19014888
HEK293 Function assay Displacement of [125I]RTI55 from human recombinant DAT expressed in HEK293 cells, Ki=6.67μM 19014888
HEK293 Function assay Inhibition of [3H]DA from human recombinant DAT expressed in HEK293 cells, IC50=19.5μM 19014888
HEK293 Function assay Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells by scintillation counting, Ki=0.0011μM 19256502
HEK293 Function assay Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting, IC50=0.0073μM 19256502
HEK293 Function assay Displacement of [3H]norepinephrine from human recombinant NET expressed in HEK293 cells by scintillation counting, IC50=1.02μM 19256502
HEK293 Function assay Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting, Ki=1.56μM 19256502
HEK293 Function assay Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells by scintillation counting, Ki=6.67μM 19256502
HEK293 Function assay Displacement of [3H]dopamine from human recombinant DAT expressed in HEK293 cells by scintillation counting, IC50=19.5μM 19256502
JAR Function assay Inhibition of serotonin uptake at human SERT expressed in human JAR cells, IC50=0.01μM 19329313
MDCK-Net6 Function assay Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells, IC50=0.563μM 19329313
JAR Function assay Inhibition of serotonin uptake at human SERT expressed in JAR cells, IC50=0.0094μM 19632110
JAR Function assay Inhibition of human SERT expressed in JAR cells, IC50=0.0094μM 19713106
JAR Function assay Inhibition of [3H]hydroxytryptamine creatinine sulfate uptake at human SERT expressed in human JAR cells, IC50=0.0094μM 19722525
HEK293 Function assay Displacement of [I125]RTI-55 from human SERT transfected in human HEK293 cells, IC50=0.0025μM 20034793
JAR Function assay Inhibition of serotonin uptake at human SERT expressed in human JAR cells, IC50=0.0094μM 20131864
JAR Function assay Inhibition of human SERT expressed in human JAR cells, IC50=0.0094μM 20378347
JAR Function assay Inhibition of SERT-mediated serotonin uptake in human JAR cells, IC50=0.0094μM 20462211
BESM Antitrypanosomal assay 88 hrs Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=7μM 20547819
BESM Cytotoxicity assay 88 hrs Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=16μM 20547819
HEK293 Function assay Displacement of [3H] astemizole from human recombinant ERG channel expressed in HEK293 cells, IC50=3.1μM 20637635
HEK293 Function assay Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells, IC50=0.0031μM 20724153
HEK293 Function assay Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting, IC50=0.0052μM 21093273
LLC-PK1 Function assay Inhibition of [3H]serotonin reuptake at human recombinant SERT expressed in LLC-PK1 cells by liquid scintillation counting, IC50=0.005012μM 21310612
HEK293 Function assay Inhibition of serotonin reuptake at SERT expressed in HEK293 cells, IC50=0.005012μM 21739935
JAR Function assay Inhibition of human SERT expressed in JAR cells assessed as serotonin uptake, IC50=0.0094μM 21916421
HEK293 Function assay Inhibition of human SERT-mediated serotonin reuptake in HEK293 cells, EC50=0.0027μM 21927645
CHO Function assay Inhibition of rat voltage-gated K channel 3.1 expressed in CHO cells by patch clamp assay, IC50=13.1μM 23121096
HEK293 Function assay 60 mins Displacement of [3H]Paroxetine from human recombinant SERT expressed in HEK293 cells after 60 mins, Ki=0.0014μM 23403082
HEK293 Function assay 60 mins Displacement of [3H]Paroxetine from human recombinant SERT expressed in HEK293 cells after 60 mins, IC50=0.0086μM 23403082
HEK293 Function assay 10 mins Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, Ki=0.098μM 23602445
HEK293 Function assay 10 mins Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, IC50=0.28184μM 23602445
HEK293 Function assay 10 mins Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, Ki=1.394μM 23602445
HEK293 Function assay 10 mins Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, Ki=3.764μM 23602445
HEK293 Function assay 10 mins Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, IC50=6.30957μM 23602445
HEK293 Function assay 10 mins Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay, IC50=9.12011μM 23602445
HEK293 Function assay Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells, IC50=0.0072μM 24012181
HEK293 Function assay 15 mins Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay, IC50=0.15μM 24974340
HEK293 Function assay 15 mins Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay, IC50=4.41μM 24974340
HEK293 Function assay 15 mins Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay, IC50=18.4μM 24974340
HEK293 Function assay 15 mins Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay, IC50=0.15μM 25221656
HEK293 Function assay 15 mins Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay, IC50=4.41μM 25221656
HEK293 Function assay 15 mins Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay, IC50=18.4μM 25221656
HEK293 Function assay Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents, IC50=14μM 26588045
tsA201 Function assay Inhibition of of human TREK1 expressed in tsA201 cells assessed as reduction in channel currents, IC50=19μM 26588045
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
RD Antiviral assay 5 mins Antiviral activity against Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth, EC50=1μM 30912944
RD Cytotoxicity assay 3 days Cytotoxicity against human RD cells after 3 days by neutral red dye-based photometric method, CC50=11.9μM 30912944
Huh7 Antiviral assay Antiviral activity against DENV2 infected in human Huh7 cells by qRT-PCR analysis, IC50=0.38μM 31128447
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 345.79 Formel

C17H18F3NO.HCl

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 56296-78-7 SDF herunterladen Lagerung von Stammlösungen

Synonyme Lilly 110140 HCl, LY-110140 HCl Smiles CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl

Löslichkeit

In vitro
Charge:

DMSO : 69 mg/mL (199.54 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC50/Ki
5-HT
In vitro

Fluoxetine blockiert die Herunterregulierung der Zellproliferation, die durch unentrinnbaren Schock (IS) von Hippocampuszellen hervorgerufen wird.

Fluoxetine erhöht die Anzahl der neugeborenen Zellen im Gyrus dentatus des Hippocampus von erwachsenen Ratten. Fluoxetine erhöht auch die Anzahl der proliferierenden Zellen im prälimbischen Kortex.

Fluoxetine beschleunigt die Reifung unreifer Neuronen. Fluoxetine verbessert die Neurogenese-abhängige Langzeitpotenzierung (LTP) im Gyrus dentatus.

Fluoxetine, aber nicht Citalopram, Fluvoxamin, Paroxetin und Sertralin, erhöht die extrazellulären Noradrenalin- und Dopaminspiegel im präfrontalen Kortex. Fluoxetine erzeugt nach akuter systemischer Verabreichung robuste und anhaltende Erhöhungen der extrazellulären Noradrenalin- und Dopaminkonzentrationen.

In vivo

Fluoxetine-Behandlung kehrt auch das Defizit in der Fluchtlatenz um, das bei Tieren beobachtet wurde, die einem unentrinnbaren Schock bei erwachsenen männlichen Sprague–Dawley-Ratten ausgesetzt waren.

Fluoxetine in Kombination mit Olanzapin führt zu robusten, anhaltenden Erhöhungen der extrazellulären Dopamin ([DA](ex))- und Noradrenalin ([NE](ex))-Spiegel um bis zu 361 % bzw. 272 % des Ausgangswertes, die signifikant größer sind als die der Einzelsubstanzen.

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/11919662/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10942849/
  • [6] https://pubmed.ncbi.nlm.nih.gov/33441923/

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT05634707 Recruiting
Primary Brain Tumor|Brain Tumor Recurrent
Duke University
 August 5 2023 Early Phase 1
NCT04676139 Unknown status
Nocturnal Enuresis
Mansoura University
 July 1 2020 Phase 3
NCT01615055 Withdrawn
Cognitive Dysfunction
University of California Los Angeles|City of Hope Medical Center
 June 2018 Early Phase 1
NCT03390933 Completed
Depression|Hemodialysis-Induced Symptom
MetroHealth Medical Center
 March 1 2018 Phase 4

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