Citalopram HBr

製品コードS4749 バッチS474903

印刷

化学情報

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 (warmed with 50ºC water bath)

81 mg/mL (199.85 mM)

Water (warmed with 50ºC water bath)

81 mg/mL (199.85 mM)

Ethanol (warmed with 50ºC water bath)

81 mg/mL (199.85 mM)

体内（毎回新しく調製した物を用意してください）

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.000mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	抗うつ薬であるCitalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr) は、IC50が1.8 nMの経口投与選択的セロトニン再取り込み阻害薬 (SSRI) です。
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. 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.
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.

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.

参考

https://pubmed.ncbi.nlm.nih.gov/6128769/
https://pubmed.ncbi.nlm.nih.gov/10633492/
https://pubmed.ncbi.nlm.nih.gov/26431045/

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：

SSRI antidepressant citalopram reverses the Warburg effect to inhibit hepatocellular carcinoma by directly targeting GLUT1 [ Cell Rep, 2024, 43(10):114818]	PubMed: 39388353
Inhibition of human UDP-glucuronosyltransferase (UGT) enzymes by darolutamide: Prediction of in vivo drug-drug interactions [ Chem Biol Interact, 2024, 403:111246]	PubMed: 39278459
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。