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Submit ReviewPK 11195
Description: Antagonist at peripheral benzodiazepine receptors
Chemical Name: 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity 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).
Technical Data for PK 11195
| M. Wt | 352.86 |
| Formula | C21H21ClN2O |
| Storage | Store at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for PK 11195
References for PK 11195
References are publications that support the biological activity of the product.
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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Keywords: PK 11195, PK 11195 supplier, antagonists, peripheral, benzodiazepine, receptors, GABAA, Receptors, PK11195, PBR, TSPO, Constitutive, Androstane, Receptor, Translocator, Protein, 0670, Tocris Bioscience
3 Citations for PK 11195
Citations are publications that use Tocris products. Selected citations for PK 11195 include:
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
Reviews for PK 11195
Average Rating: 5 (Based on 1 Review.)
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A peripheral benzodiazepine receptor (PBR) agonist..
By
Anonymous on 05/02/2018
Assay Type: In Vitro
Species: 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.