Quetiapine Fumarate 是5-HT受体激动剂和多巴胺受体拮抗剂，对人5-HT1A和人D2的pEC50值分别为 4.77 和 6.33，具有抗抑郁和抗焦虑作用。

Quetiapine Fumarate, an atypical antipsychotic, is used in the treatment of bipolar I mania, schizophrenia, bipolar II depression, bipolar I depression.

Quetiapine改变大脑边缘神经降压素神经递质和c-fos表达.Quetiapine还有抗精神病活性,减少引起锥体外系症状和持续增加催乳素的倾向.Quetiapine在行为和生物化学试验的活性与clozapine类似,并可能具有神经保护性质.

Quetiapine具有多巴胺-2受体和clozapine亲和力,且对各种神经递质受体,包括血清素,组胺,多巴胺和肾上腺素能受体具有相近的亲合性。

CDK activity assays: CDK assays for IC50 determinations and kinetic evaluation are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST?RB-Cterm). The total reaction volume is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST?RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-32P]ATP are added to the wells, and placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP, and incubated at 25℃ for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid, and the plate is kept at 4?℃ for at least 1 hr to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% trichloroacetic acid, and radioactive incorporation is determined with a β plate counter.

111974-72-2

C46H54N6O8S2

883.09

Quetiapine Fumarate;富马酸喹硫平;ICI-204636;Quetiapine hemifumarate

DMSO:22.1 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years