Fluoxetine HCl

別名: Lilly 110140 HCl, LY-110140 HCl 中文名稱：鹽酸氟西汀

目錄號(hào)：S1333 Purity: 99.95%

Fluoxetine HCl是一種抗抑郁劑，選擇性抑制5-羥色胺再攝取。

Fluoxetine HCl Chemical Structure

CAS: 56296-78-7

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	997	現(xiàn)貨
10mg	794.43	現(xiàn)貨
25mg	1217.77	現(xiàn)貨
100mg	2446.52	現(xiàn)貨
1g	8763.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.95%

99.95

Fluoxetine HCl相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	5-HT1 5-HT2 5-HT3 5-HT4 5-HT6 5-HT7 5-HT5	點(diǎn)擊展開(kāi)
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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
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	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	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
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
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
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		Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells, IC50=0.0072μM	24012181
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
Huh7	Antiviral assay		Antiviral activity against DENV2 infected in human Huh7 cells by qRT-PCR analysis, IC50=0.38μM	31128447
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生物活性

產(chǎn)品描述

Fluoxetine HCl是一種抗抑郁劑，選擇性抑制5-羥色胺再攝取。

靶點(diǎn)

5-HT ^[1]

體外研究(In Vitro)
體外研究活性	Fluoxetine阻斷細(xì)胞增殖的下調(diào)，導(dǎo)致海馬細(xì)胞的不可避免的沖擊（IS）。^[1] Fluoxetine增加成年大鼠的海馬的齒狀回的新生細(xì)胞的數(shù)量。Fluoxetine也增加了前度皮質(zhì)的增殖細(xì)胞的數(shù)目。^[2] Fluoxetine加速未成熟神經(jīng)元的成熟。Fluoxetine增強(qiáng)海馬齒狀回的神經(jīng)依賴的長(zhǎng)時(shí)程增強(qiáng)（LTP）。^[3] Fluoxetine而不是Citalopram, Fluvoxamine, Paroxetine和Sertraline，增加前額葉皮層中去甲腎上腺素和多巴胺的細(xì)胞外水平。在急性全身給藥后，Doxazosin產(chǎn)生強(qiáng)勁而持續(xù)增加的去甲腎上腺素和多巴胺的胞外濃度。^[4]

體外研究(In Vitro)

體外研究活性

Fluoxetine阻斷細(xì)胞增殖的下調(diào)，導(dǎo)致海馬細(xì)胞的不可避免的沖擊（IS）。^[1]

Fluoxetine增加成年大鼠的海馬的齒狀回的新生細(xì)胞的數(shù)量。Fluoxetine也增加了前度皮質(zhì)的增殖細(xì)胞的數(shù)目。^[2]

Fluoxetine加速未成熟神經(jīng)元的成熟。Fluoxetine增強(qiáng)海馬齒狀回的神經(jīng)依賴的長(zhǎng)時(shí)程增強(qiáng)（LTP）。^[3]

Fluoxetine而不是Citalopram, Fluvoxamine, Paroxetine和Sertraline，增加前額葉皮層中去甲腎上腺素和多巴胺的細(xì)胞外水平。在急性全身給藥后，Doxazosin產(chǎn)生強(qiáng)勁而持續(xù)增加的去甲腎上腺素和多巴胺的胞外濃度。^[4]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在動(dòng)物成年雄性SD大鼠中，F(xiàn)luoxetine扭轉(zhuǎn)不可避免的沖擊導(dǎo)致的逃避潛伏期。^[1] 在動(dòng)物成年雄性SD大鼠中，F(xiàn)luoxetine和Olanzapine聯(lián)用產(chǎn)生穩(wěn)健，持續(xù)的細(xì)胞外多巴胺水平（[DA]（前））和去甲腎上腺素（[東北]（前））的增加，超過(guò)基準(zhǔn)達(dá)361％和272％，這是顯著大于兩種藥物單獨(dú)使用。^[5]

體內(nèi)研究(In Vivo)

體內(nèi)研究活性

在動(dòng)物成年雄性SD大鼠中，F(xiàn)luoxetine扭轉(zhuǎn)不可避免的沖擊導(dǎo)致的逃避潛伏期。^[1]

在動(dòng)物成年雄性SD大鼠中，F(xiàn)luoxetine和Olanzapine聯(lián)用產(chǎn)生穩(wěn)健，持續(xù)的細(xì)胞外多巴胺水平（[DA]（前））和去甲腎上腺素（[東北]（前））的增加，超過(guò)基準(zhǔn)達(dá)361％和272％，這是顯著大于兩種藥物單獨(dú)使用。^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[1] Malberg JE, et al. Neuropsychopharmacology, 2003, 28(9), 1562-1571. [2] Kodama M, et al. Biol Psychiatry, 2004, 56(8), 570-580. [3] Wang JW, et al. J Neurosci, 2008, 28(6), 1374-1384. [4] Bymaster FP, et al. Psychopharmacology (Berl), 2002, 160(4), 353-361. [5] Zhang W, et al. Neuropsychopharmacology, 2000, 23(3), 250-262. [6] Stapel B, et al. Sci Rep. 2021 Jan 13;11(1):1250. + 展開(kāi)

參考文獻(xiàn)

[1] Malberg JE, et al. Neuropsychopharmacology, 2003, 28(9), 1562-1571.
[2] Kodama M, et al. Biol Psychiatry, 2004, 56(8), 570-580.
[3] Wang JW, et al. J Neurosci, 2008, 28(6), 1374-1384.

[4] Bymaster FP, et al. Psychopharmacology (Berl), 2002, 160(4), 353-361.
[5] Zhang W, et al. Neuropsychopharmacology, 2000, 23(3), 250-262.
[6] Stapel B, et al. Sci Rep. 2021 Jan 13;11(1):1250.

+ 展開(kāi)