MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

SKF-83566

CAS No. : 99295-33-7

MCE 国际站：SKF-83566

产品活性：SKF-83566 是一种有效的，可通透血脑屏障的，具有口服活性的 D1 样多巴胺受体 ( D1-like dopamine receptor) 拮抗剂，也可以作为一种较弱的竞争性拮抗剂，作用于血管 5-HT₂ 受体 (K_i =11 nM)。SKF-83566 是一种竞争性多巴胺转运蛋白 (DAT) 抑制剂，IC₅₀ 为 5.7 μM。在离体兔胸主动脉中，SKF-83566 对腺苷基环化酶 2 (AC₂) 的选择性高于对 AC₁ 和 AC₅ 的。SKF-83566 可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor  |  5-HT Receptor  |  Adenylate Cyclase

In Vitro: SKF-83566 (0.1 μM-10 μM) causes a concentration-dependent increase in peak evoked extracellular DA concentration ([DA]_o)?evoked by single-pulse stimulation, with a maximum 65% increase in peak evoked [DA]_o with 5 μM. The EC₅₀ value of this effect of SKF-83566 is 1.3 μM.
SKF-83566 inhibited [³H]DA uptake with an IC₅₀?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [³H]CFT, with an IC₅₀?of 0.51 μM in [³H]DA uptake and [³H]CFT binding studies.
Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [³H]CFT binding with an IC₅₀?of 0.77 μM in LLc-PK-rDAT cell membrane preparations.

In Vivo: SKF 83566 (oral administration; 20 μg/mL; 7 days) alone has no effects on altering LTP (115%). However, combinnation of SKF 83566 and nicotine significantly blocks the enhancement of long-term synaptic potentiation (LTP) induced by pretreatment with nicotine (SKF 83566+nicotine+cocaine, 120%; nicotine+cocaine, 143%).

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  CNS-Penetrant Compound Library  |  Neurotransmitter Receptor Compound Library  |  Anti-Alzheimer's Disease Compound Library  |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Targeted Diversity Library  |  5-HT Receptor Compound Library  |  Coagulation and Anti-coagulation Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  SB 243213  |  Perphenazine-d₈ dihydrochloride  |  (Rac)-SEP-363856  |  Small Cardioactive Peptide B (SCPB)  |  Bromperidol-d₄-1  |  Haloperidol  |  Loxapine-d₈ hydrochloride  |  ARC 239  |  Ondansetron-d₃  |  PG01037 dihydrochloride  |  Zotepine  |  Paliperidone-d₄  |  Dehydroaripiprazole  |  Nuciferine  |  Preclamol hydrochloride  |  Sonepiprazole  |  Ziprasidone hydrochloride monohydrate  |  WAY-100635 Maleate  |  Velusetrag  |  (S)-Mirtazapine  |  Eletriptan  |  CY 208-243  |  Pindolol-d₇  |  Paliperidone palmitate  |  p-MPPI hydrochloride  |  Raclopride tartrate  |  Trifluoperazine dihydrochloride  |  LY 344864 racemate  |  Paliperidone  |  LY-272015 hydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。