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Submit ReviewPK 11195
说明： Antagonist at peripheral benzodiazepine receptors
化学名： 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for PK 11195
PK 11195 has high affinity for the peripheral benzodiazepine receptor (PBR, TSPO) without binding to other known neurotransmitter receptors. Also inhibits the human constitutive androstane receptor (hCAR).
技术数据 for PK 11195
| 分子量 | 352.86 |
| 公式 | C21H21ClN2O |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 85532-75-8 |
| PubChem ID | 1345 |
| InChI Key | RAVIZVQZGXBOQO-UHFFFAOYSA-N |
| Smiles | CCC(C)N(C)C(=O)C1=NC(C2=CC=CC=C2Cl)=C2C=CC=CC2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for PK 11195
参考文献 for PK 11195
参考文献是支持产品生物活性的出版物。
Conway et al (1998) Temporal changes in glial fibrillary acidic protein messenger RNA and [3H]PK11195 binding in relation to imidazoline-I2-receptor and α2-adrenoceptor binding in the hippocampus following transient global forebrain isch Neuroscience 82 805 PMID: 9483537
Le Fur et al (1983) Differentiation between two ligands for peripheral benzodiazpine binding sites [3H]-Ro 5-4864 and [3H]-PK11195, by thermodynamic studies. Life Sci. 33 449 PMID: 6308375
Li et al (2008) The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human androstane receptor. Mol.Pharmacol. 74 443 PMID: 18492798
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关键词: PK 11195, PK 11195 supplier, antagonists, peripheral, benzodiazepine, receptors, GABAA, Receptors, PK11195, PBR, TSPO, Constitutive, Androstane, Receptor, Translocator, Protein, 0670, Tocris Bioscience
3 篇 PK 11195 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PK 11195 的部分引用包括：
Gut et al (2013) Whole-organism screening for gluconeogenesis identifies activators of fasting metabolism. J Cell Mol Med 9 97 PMID: 23201900
Anderson et al (2011) Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR). Toxicol Lett 202 148 PMID: 21315811
Sutter et al (2003) Ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in oesophageal cancer cells: involvement of the p38MAPK signalling pathway. Nat Chem Biol 89 564 PMID: 12888831
PK 11195 的评论
平均评分: 5 (Based on 1 Review.)
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A peripheral benzodiazepine receptor (PBR) agonist..
By
Anonymous on 05/02/2018
分析类型： In Vitro
种属： Human
It is a peripheral benzodiazepine receptor (PBR) agonist. It is effective in inhibiting LPS-induced pro-inflammatory cytokines such as IL-1beta and TNF-alpha in microglia culture.