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Fluoxetine HCl 5-HT Receptor remmer

Name: Fluoxetine HCl
Brand: Selleck Chemicals
SKU: S1333
Rating: 5 (22 reviews)

Cat.Nr.S1333

Fluoxetine HCl is een selectieve serotonine-heropnameremmer (SSRI) ter hoogte van de neuronale membraan, gebruikt bij de behandeling van depressie.

Fluoxetine HCl 5-HT Receptor remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 345.79

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Kwaliteitscontrole

Batch: Zuiverheid: 99.94%

99.94

Gerelateerde doelwitten	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Overige 5-HT Receptor Inhibitoren	WAY-100635 Maleate Serotonin (5-HT) HCl Puerarin BRL-15572 Dihydrochloride SB269970 HCl Ketanserin RS-127445 Nuciferine Flopropione BRL-54443

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	345.79	Formule	C₁₇H₁₈F₃NO.HCl	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	56296-78-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	Lilly 110140 HCl, LY-110140 HCl			Smiles	CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl

Oplosbaarheid

In vitro
Batch:

DMSO : 69 mg/mL (199.54 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

DMSO : 69 mg/mL (199.54 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 69 mg/mL

Water : 25 mg/mL (超声加热五分钟)

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	5-HT
In vitro	Fluoxetine blokkeert de downregulatie van celproliferatie als gevolg van onvermijdelijke schok (IS) van hippocampale cellen. Fluoxetine verhoogt het aantal pasgeboren cellen in de gyrus dentatus van de hippocampus van volwassen ratten. Fluoxetine verhoogt ook het aantal prolifererende cellen in de prelimbische cortex. Fluoxetine versnelt de rijping van onvolgroeide neuronen. Fluoxetine verbetert de neurogenese-afhankelijke langetermijnpotentiëring (LTP) in de gyrus dentatus. Fluoxetine, maar niet citalopram, fluvoxamine, paroxetine en sertraline, verhoogt de extracellulaire niveaus van noradrenaline en dopamine in de prefrontale cortex. Fluoxetine produceert robuuste en aanhoudende verhogingen van de extracellulaire concentraties van noradrenaline en dopamine na acute systemische toediening.
In vivo	Fluoxetine behandeling keert ook het tekort in ontsnappingslatentie om dat wordt waargenomen bij dieren die zijn blootgesteld aan onvermijdelijke schok bij volwassen mannelijke Sprague–Dawley ratten. Fluoxetine gecombineerd met Olanzapine produceert robuuste, aanhoudende verhogingen van extracellulaire niveaus van dopamine ([DA](ex)) en noradrenaline ([NE](ex)) tot respectievelijk 361% en 272% van de basislijn, die significant groter zijn dan die van elk medicijn afzonderlijk.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/12838272/ [2] https://pubmed.ncbi.nlm.nih.gov/15476686/ [3] https://pubmed.ncbi.nlm.nih.gov/18256257/ [4] https://pubmed.ncbi.nlm.nih.gov/11919662/ [5] https://pubmed.ncbi.nlm.nih.gov/10942849/ [6] https://pubmed.ncbi.nlm.nih.gov/33441923/

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

Technische ondersteuning

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Tel: +1-832-582-8158 Ext:3

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