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Fluoxetine HCl 5-HT Receptor inibitore

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

N. Cat.S1333

Fluoxetine HCl è un inibitore selettivo della ricaptazione della serotonina (SSRI) a livello della membrana neuronale, utilizzato nel trattamento della depressione.

Fluoxetine HCl 5-HT Receptor inibitore Chemical Structure

Struttura chimica

Peso molecolare: 345.79

Vai a

Controllo Qualità

Lotto: Purezza: 99.94%

99.94

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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	345.79	Formula	C₁₇H₁₈F₃NO.HCl	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	56296-78-7	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Lilly 110140 HCl, LY-110140 HCl			Smiles	CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl

Solubilità

In vitro
Lotto:

DMSO : 69 mg/mL (199.54 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

DMSO : 69 mg/mL (199.54 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 69 mg/mL

Water : 25 mg/mL (超声加热五分钟)

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	5-HT
In vitro	Fluoxetine blocca la down-regulation della proliferazione cellulare risultante da shock inevitabile (IS) delle cellule ippocampali. Fluoxetine aumenta il numero di cellule neonatali nel giro dentato dell'ippocampo di ratto adulto. Fluoxetine aumenta anche il numero di cellule proliferanti nella corteccia prelimbica. Fluoxetine accelera la maturazione dei neuroni immaturi. Fluoxetine migliora la potenziale a lungo termine (LTP) dipendente dalla neurogenesi nel giro dentato. Fluoxetine, ma non citalopram, fluvoxamina, paroxetina e sertralina, aumenta i livelli extracellulari di noradrenalina e dopamina nella corteccia prefrontale. Fluoxetine produce aumenti robusti e sostenuti delle concentrazioni extracellulari di noradrenalina e dopamina dopo somministrazione sistemica acuta.
In vivo	Il trattamento con Fluoxetine inverte anche il deficit di latenza di fuga osservato in animali esposti a shock inevitabile in ratti Sprague–Dawley maschi adulti. Fluoxetine combinata con Olanzapine produce aumenti robusti e sostenuti dei livelli extracellulari di dopamina ([DA](ex)) e noradrenalina ([NE](ex)) fino al 361% e al 272% del valore basale, rispettivamente, che sono significativamente maggiori rispetto a ciascun farmaco da solo.
Riferimenti	[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/

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Supporto tecnico

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