富马酸喹硫平 T6241

Product Introduction
Bioactivity


英文名: Quetiapine hemifumarate

描述: Quetiapine hemifumarate (ICI-204636) 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。

激酶实验: 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.

体外活性: 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.

体内活性: 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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (28.31 mM)


关键字: Quetiapine Hemifumarate | Quetiapine hemifumarate | 5-hydroxytryptamine Receptor | Inhibitor | Quetiapine | anxiolytic | 5-HT Receptor | inhibit | Antidepressant | 5-HT2A | 5-HT1A | Serotonin Receptor | 5-HT2C | ICI204636 | Dopamine Receptor | ICI 204636

相关产品: Dasotraline hydrochloride | Tiospirone | Tetrabenazine | Nomifensine maleate | FAUC 213 | PG 01037 dihydrochloride | Hirsuteine | Pramipexole dihydrochloride | (+)-PD 128907 hydrochloride | PNU-96391

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Neurotransmitter Receptor Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Preclinical Compound Library

富马酸喹硫平 T6241信息由TargetMol中国为您提供，如您想了解更多关于富马酸喹硫平 T6241报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途