Quetiapine Fumarate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Quetiapine hemifumarate 是一种 5-HT 受体激动剂，对人 5-HT1A 的 pEC50 值为 4.77。Quetiapine hemifumarate 是多巴胺受体 (dopamine receptor) 拮抗剂，对人 D2 的 pIC50 值为 6.33。Quetiapine hemifumarate 对人 D2，HT1A，5-HT2A，5-HT2C 受体具有中高等亲和力，pKi 值为 7.25，5.74，7.54，5.55。具有抗抑郁和抗焦虑作用。

Quetiapine Fumarate is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.(In Vitro):Quetiapine (<100?μM; 24?hours) has no significant effect on cell viabilities.Quetiapine (10?μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner.Quetiapine (10?μM) also inhibits TNF-α synthesis.(In Vivo):Quetiapine (10?mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination.

Quetiapine (<100?μM; 24?hours) has no significant effect on cell viabilities.Quetiapine (10?μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner. Quetiapine (10?μM) also inhibits TNF-α synthesis. Cell Viability Assay Cell Line:N9 microglial cells Concentration:0, 0.1, 1, 10, 50, and 100?μM Incubation Time:24?hours Result:Had no significant effect on cell viabilities at various concentrations under 100?μM, in which significant toxicity could be observed. RT-PCR Cell Line:N9 microglial cells Concentration:10?μM Incubation Time:24?hours Result:Dramatically inhibited TNF-α synthesis.

Quetiapine (10?mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination. Animal Model:C57BL/6 mice Dosage:10?mg/kg/day Administration:Ingested Result:Significantly increased in optical density of myelin basic protein (MBP) staining compared to Veh group.

ICI 204636

Endocrinology/Hormones

5-HT Receptor

HT| Adrenergic Receptor| Dopamine

Neurological Disease

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111974-72-2

883.09

C46H54N6O8S2

>98% (HPLC)

DMSO: 36 mg/mL (40.76 mM)

C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42.C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42.C(=C/C(=O)O)\C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years