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靶点:Serotonin Transporter 通路:Neuronal Signaling 背景说明:是一种选择性血清素再摄取抑制剂 (SSRI),抑制 5-HT 摄取进入突触体。 生物活性:Citalopram Hydrobromide 是一种新的双环酞烷衍生物,是神经元血清素(5-HT)摄取的强效抑制剂,IC50 为 1.8 nM。可抑制兔血小板对 5-HT 的摄取,IC50 为 14 nM。抗抑郁作用。[1] In Vitro:Citalopram and escitalopram showed concentration-dependent cytotoxicity on 2 non-MYCN amplified cell lines(rat B104 and human SH-SY5Y)and 2 human MYCN amplified cell lines(IMR32 and Kelly). Citalopram was more cytotoxic than escitalopram. IMR32 was the most sensitive cell line.[2] In Vivo:In the Spontaneously Hypertensive rats(SHRs),Lewis(LEW)rats,and Wistar-Kyoto(WKY)rats,citalopram(1-10 mg/kg,i.p.)pretreatment increased central 5-HT levels and/or decreased 5-hydroxyindoleacetic acid levels.[3] 动物实验:Acute administration of the selective serotonin(5-HT)reuptake inhibitor(SSRI),citalopram(1-10 mg/kg,i.p. 1 h before an elevated plus-maze test),to Spontaneously Hypertensive rats(SHRs),Lewis(LEW)rats,and Wistar-Kyoto(WKY)rats,i.e.,rat strains differing for their emotionality,promoted anxiety,and/or hypoactivity,except in WKY rats.[3] 数据来源文献:[1]. Hyttel J. Citalopram--pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity. Prog Neuropsychopharmacol Biol Psychiatry. 1982;6(3):277-95. [2]. Sakka L,et al. Assessment of citalopram and escitalopram on neuroblastoma cell lines. Cell toxicity and gene modulation. Oncotarget. 2017 Jun 27;8(26):42789-42807. [3]. Pollier F,et al. Serotonin reuptake inhibition by citalopram in rat strains differing for their emotionality. Neuropsychopharmacology. 2000 Jan;22(1):64-76.
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| 其它标识: |
EC:EINECS 261-890-6 MDL:MFCD02101306 SMILES:CN(C)CCCC1(C2=C(CO1)C=C(C=C2)C#N)C3=CC=C(C=C3)F.Br InChIKey:WIHMBLDNRMIGDW-UHFFFAOYSA-N InChI:InChI=1S/C20H21FN2O.BrH/c1-23(2)11-3-10-20(17-5-7-18(21)8-6-17)19-9-4-15(13-22)12-16(19)14-24-20;/h4-9,12H,3,10-11,14H2,1-2H3;1H PubChem CID:77995
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| 基本信息: |
CAS:59729-32-7 中文名称:氢溴酸西肽普兰 英文名称:Citalopram Hydrobromide 别名:Prepram HBr;Bonitrile HBr;Citalopram HBr;Lu 10-171;XU-62-320;Nitalapram HBr;(±)-Citalopram hydrobromide 分子式:C20H22BrFN2O 分子量:405.3 规格:10mg ; 25mg 溶解性:Soluble in Water/DMSO(Need ultrasonic) 纯度:≥98% 外观(性状):White to off-white Solid 储存条件:Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
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| 靶点: |
Serotonin Transporter |