化学性质:
规格 | 10mM (in 1mL DMSO) 1g 5g |
CAS | 111974-72-2 |
别名 |
|
化学名 | 2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol;(E)-but-2-enedioic acid |
分子式 | C46H54N6O8S2 |
分子量 | 883.09 |
溶解度 | ≥ 11.03mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
Quetiapine Fumarate is a novel atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression and bipolar I depression [1]. The antipsychotic effect of quetiapine might be mediated through antagonist activity at dopamine and serotonin receptors. Quetiapine specifically antagonized the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adreno-receptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes[1].
In vitro: Quetiapine has shown affinity for various neurotransmitter receptorsincluding dopamine, serotonin, histamine, and adrenergicreceptors, Quetiapine exihibited binding characteristics at the dopamine-2receptorsimilar to those of clozapine [1].
In vivo: In animal models, Quetiapine exihibited a preclinical profile suggestive of antipsychotic activity with a reduced tendency to cause extrapyramidal symptoms (EPS) and sustained prolactin elevation. Quetiapine altered neurotensin neurotransmission and c-fos expression in limbic but not motor brain regions.In humans, quetiapine exhibited linear pharmacokinetics with a mean terminal half-life of 7 hours.The optimal dosing range for quetiapine was 150 to 750 mg/day, and recent results suggested that once-daily dosing might be suitable for some patients [1].Quetiapine prevented schizophrenia and depression in hippocampal cell proliferation and BDNF expression caused by chronic restraint stress (CRS) in rats in a dose-dependent manner. Quetiapine (5 mg/kg) in combination with venlafaxine (2.5 mg/kg) increaseed hippocampal cell proliferation and prevented BDNF decrease in stressed rats, while each of the drugs exerted mild or no effects [2].In rats subjected to chronic-restraint stress, chronic administration of quetiapine attenuated the decrease in levels of brain-derived neurotrophic factor (BDNF) in the hippocampi. The stress-induced suppression of hippocampal neurogenesis was reversed after post-stress administration of quetiapine (10 mg/kg) for 7 or 21 days, evidenced in the numbers of pCREB-positive and BrdU-labeled cells that were comparable to those in non-stressed rats but higher than those in the vehicle-treated rats [3].
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