PK 11195 (PK11195)

10/01/2013 - "In the present study, we showed that glial activation could be quantitatively imaged in the spinal cord of neuropathic pain rats using [(11)C]PK11195 PET, suggesting that high resolution PET using TSPO-specific radioligands might be useful for imaging to assess the role of glial activation, including neuroinflammatory processes, in neuropathic pain patients."
05/01/2009 - "In the present study, we first tested whether the enhanced PBR expression is causally related to neuropathic pain, and we found that the PBR antagonist PK11195 is effective in reducing SNL-induced mechanical allodynia and thermal hyperalgesia. "
05/01/2013 - "Using radioligand binding autoradiography and filtration assays, we examined the specific binding of the PBR/TSPO ligand [(3)H]PK11195 in spinal cords from the following rat experimental pain models: neuropathic pain induced by spinal nerve ligation (SNL), osteoarthritic pain induced by intraarticular injection of monosodium iodoacetate in the knee joint (MIA-OA), and subchronic inflammatory pain induced by intraplantar injection of complete Freund's adjuvant (CFA). "

06/25/1984 - "At these doses PK 11195 alone does not modify the sensitivity to audiogenic seizures, but at doses between 20-80 mg/kg it protects DBA/2J mice against audiogenic seizures. "
12/10/1999 - "[11C](R)-PK11195 PET was carried out in four normal subjects, two patients with histologically confirmed RE, and three patients with clinically stable hippocampal sclerosis and low seizure frequency. "
04/22/1996 - "PK 11195 (i.v.), a specific antagonist for PBR, raised seizure thresholds of EL mice at a dose of 2 mg/kg. Binding assay revealed a 50% higher density of [3H]Ro 5-4864 binding sites in the mitochondrial fraction isolated from the cerebrum of EL mice in comparison with DDY mice. "
01/01/1995 - "PK 11195 reduces the brain availability of lindane in rats and the convulsions induced by this neurotoxic agent."
05/01/1993 - "Seizure threshold was reduced at 4 days after lorazepam discontinuation; this effect was attenuated by coadministration of PK11195 at 5 mg/kg per day. "

05/01/2009 - "In the present study, we first tested whether the enhanced PBR expression is causally related to neuropathic pain, and we found that the PBR antagonist PK11195 is effective in reducing SNL-induced mechanical allodynia and thermal hyperalgesia. "
01/01/2016 - "A single intrathecal injection of TSPO agonist Ro5-4864, but not TSPO antagonist PK11195, alleviated the mechanical allodynia in a dose-dependent manner. "

01/01/2015 - "PK11195 is a ligand for TSPO and, labelled with a positron emitter, it is also the most used tracer for PET molecular imaging to in vivo map the microglia activation in various neurological disorders, including ischemic stroke. "
11/01/2006 - "[(11)C](R)-PK11195 is a marker of activated microglia, which can be used to measure inflammation in neurologic disorders. "
01/01/2008 - "However, the potential of these new PBR ligands is still under investigation and as a consequence [(11)C]PK11195 is used so far to image activated microglia cells in neurological disorders. "
10/01/2008 - "We conclude that 1) ligands that bind peripheral benzodiazepine receptor mainly label activated microglia in human neurological disorders and that 2) DAA1106 may possess binding characteristics superior to those of PK11195, which may be beneficial for in vivo positron emission tomography imaging."

06/04/1990 - "Using radioligand binding techniques, we have demonstrated that 6 out of 6 glioblastoma (GBM) specimens had high concentrations of PBR [( 3H]PK 11195 binding sites) which were significantly greater than in 5 normal human frontal cortex samples. "
01/01/1989 - "To determine the affinity of this [125I]PK 11195 analog for human glioma cells, saturation experiments were performed on monolayers of U251 human glioblastoma cells. "
01/01/2008 - "With the aid of the dye JC-1 and cyclosporin A, applied to glioblastoma cells, we now investigated the significance of opening of the mitochondrial permeability transition pore (MPTP) for ErPC3-induced apoptosis in interaction with the TSPO ligands, PK 11195 and Ro5 4864. "