Citalopram hydrobromide
产品名称:Citalopram hydrobromide
产品描述:
产品描述 | Citalopram, a selective serotonin reuptake inhibitor (SSRI), selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). Citalopram Hydrobromide is the orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA). |
靶点活性 | serotonin reuptake:1.8 nM |
体外活性 | 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), acetylcholine, and morphine receptors. 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]. |
体内活性 | 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]. |
细胞实验 | 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.(Only for Reference) |
别名 | Lu 10-171, Lu 10-171 HBr, Bonitrile HBr, 氢溴酸西酞普兰, Nitalapram HBr, Citalopram HBr, XU-62-320 |
分子量 | 405.31 |
分子式 | C20H21FN2O·HBr |
CAS No. | 59729-32-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 6 mg/mL(14.8 mM)
H2O: 4 mg/mL(9.9 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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