Chemical Name: 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Biological ActivityPossesses high affinity for the peripheral benzodiazepine receptor (PBR, TSPO) without binding to other known neurotransmitter receptors. Also inhibits the human constitutive androstane receptor (hCAR).
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The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human androstane receptor.
Li et al.
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
Conway et al.
Differentiation between two ligands for peripheral benzodiazpine binding sites [3H]-Ro 5-4864 and [3H]-PK11195, by thermodynamic studies.
Le Fur et al.
Life Sci., 1983;33:449
Citations for PK 11195
The citations listed below are publications that use Tocris products. Selected citations for PK 11195 include:
3 Citations: Showing 1 - 3
Whole-organism screening for gluconeogenesis identifies activators of fasting metabolism.
Authors: Gut Et al.
J Cell Mol Med 2013;9:97
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).
Authors: Anderson Et al.
Toxicol Lett 2011;202:148
Ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in oesophageal cancer cells: involvement of the p38MAPK signalling pathway.
Authors: Sutter Et al.
Nat Chem Biol 2003;89:564
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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.