Citalopram HBr

製品コードS4749 バッチS474902

印刷

化学情報

Chemical Structure Synonyms Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H21FN2O.HBr
分子量 405.3 CAS No. 59729-32-7
Solubility (25°C)* 体外 DMSO 81 mg/mL warmed with 50ºC water bath (199.85 mM)
Water 15 mg/mL warmed with 50ºC water bath (37.0 mM)
Ethanol 6 mg/mL warmed with 50ºC water bath (14.8 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.
in vitro

Citalopram (Lu 10-171), a new bicyclic phthalane derivative, is an extremely potent inhibitor of neuronal serotonin (5-HT) uptake but has no effect on the uptake of noradrenaline(NA) and dopamine (DA) and no antagonistic activity towards 5-HT, histamine, gamma aminobutyric acid (GABA) and acetylcholine. It is an extremely specific and potent inhibitor of neuronal 5-HT uptake. Uptake mechanisms for other transmitter amines are not influenced by the drug[1]. The SSRI citalopram has a greater effect on proliferation and a lesser effect on apoptotic activity. It affects cell cycle regulation by increasing proliferative potential and decreasing apoptotic activity in a site specific manner that may be indicative of hyperplasia. Citalopram alters FGF, MSX and TGFB expression in osteoblast cell culture[3].
in vivo

Citalopram is devoid of cardiotoxic effects even when animals are exposed to concentrations far above the therapeutic level. In man citalopram is metabolized to compounds which are also potent 5-HT-uptake inhibitors without effect on noradrenaline(NA) uptake and which are found in lower concentrations than citalopram itself. Citalopram (1-16 mg/kg) stimulates the hind limb flexor reflex in the spinal rat. Citalopram potentiates 5-HT transmission~ possibly by producing very strong uptake inhibition without simultaneously blocking the post-synaptic 5-HT receptors[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MC3T3-E1 murine calvaria osteoprogenitor cells
濃度 0.1 nM-100 μM
反応時間 3 or 7 days
実験の流れ

Cells are cultured in alpha minimum Eagles medium supplemented with 1% penicillin/streptomycin, 10% fetal bovine serum and Amphotericin B. For control data, cells are cultured for 3 or 7 days with standard alpha proliferation media. For SSRI treatments, media is supplemented with citalopram eluted to serially diluted doses between 10−4 mol through 10−10 mol to achieve a dose response curve.
動物実験 動物モデル Spontaneously Hypertensive rats (SHRs), Lewis (LEW) rats, and Wistar-Kyoto (WKY) rats
投薬量 1-10 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Long-term exposure to polypharmacy impairs cognitive functions in young adult female mice [ Aging (Albany NY), 2021, 13(11):14729-14744] PubMed: 34078751
Inhibitors of Venezuelan Equine Encephalitis Virus Identified Based on Host Interaction Partners of Viral Non-Structural Protein 3 [ Viruses, 2021, 13(8)1533] PubMed: 34452398
Effect of SSRI exposure on the proliferation rate and glucose uptake in breast and ovary cancer cell lines [ Sci Rep, 2021, 11(1):1250] PubMed: 33441923
Chronic polypharmacy impairs explorative behavior and reduces synaptic functions in young adult mice [ Aging (Albany NY), 2020, 12(11):10147-10161] PubMed: 32445552
Chronic Polypharmacy Impairs Explorative Behavior and Reduces Synaptic Functions in Young Adult Mice [ Aging (Albany NY), 2020, 44187] PubMed: 32445552

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。