產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 1g 5g
CAS	111974-72-2
別名
化學(xué)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
儲(chǔ)存條件	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 All other available size: ship with RT , or blue ice upon request

產(chǎn)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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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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