The effects of PK11195, a high-affinity peripheral benzodiazepine receptor (PBR) ligand, on protein phosphorylation in isolated purified rat brain mitochondria were investigated. The isoquinoline carboxamide ligand of PBR, PK11195, but not the benzodiazepine ligand Ro5-4864, in the nanomolar ...
联系电话: 1-631-485-4226; 16314854226 电子邮件: info@bocsci.com 国籍: 美国 产品介绍: 英文名称:(R)-(-)-PK 11195CAS:205934-46-9纯度:99% 备注:(R)-(-)-PK 11195 is the (R)-enantiomer of PK 11195, which is a peripheral benzodiazepine antagonist with high affinity for PBR in all spec...
melatonin and 2-iodomelatonin, on induced AC activity.5Saturation binding studies, conducted at 30掳C with [3H]-diazepam revealed a single binding site in the rat striatum (KD = 19.3 卤 0.80 nM) which significantly decreased in affinity in the presence of GTP (KD = 30.5 卤 2.6 nM; P ...
The present data de that high affinity binding sites for peripheral type benzodiazepines are present in human iris/ciliary-body. This tissue is therefore a suitable tool for evaluation of the putative functional role of these binding sites. 展开 关键词: peripheral type benzodiazepine human iris ...
The present study was designed to investigate the effects of diazepam, a benzodiazepine (BZ) with high affinity to central BZ receptors and moderate affinity to mitochondiral BZ receptors, and of Ro 5-4864 and PK 11195, ligands specific for mitochondrial BZ receptors, on cardiac function in the...
PK 11195 is a high-affinity ligand for the PBR. The aim of this study was to investigate in humans the biodistribution and dosimetry of [ 123 I]iodo-PK 11195, a potential single-photon emission tomography tracer for the PBR. Five healthy volunteers were injected with 112MBq of [ 123 I]...
On the other hand, the binding affinity ( K d) in fibrosarcoma was lower than that in the kidney (kidney: 0.45 nM; fibrosarcoma: 1.34 nM). It is noteworthy that the in vivo binding of [ 3H]PK-11195 in fibrosarcoma increased with increasing doses of [ 3H]PK-11195 (in the dose ...
The apparent affinity was in the range of 2–6 nM in vitro, predicting high specific binding in PET studies of living brain. However, the distribution volume (Vd, ml g−1) of high specifSynapseCumming, P., Pedersen, M.D., Minuzzi, L., Mezzomo, K., Danielsen, E.H., Iversen, P...
PK 11195 is a high-affinity ligand for the PBR. The aim of this study was to investigate in humans the biodistribution and dosimetry of [[sup 123]I]iodo-PK 11195, a potential single-photon emission tomography tracer for the PBR. Five healthy volunteers were injected with 112 MBq of [[...
A decrease in the affinity for [ 3H]-PK 11195 (a new ligand for the peripheral type benzodiazepine binding sites) was also observed. Pharmacological specificity of displacing agents was conserved during solubilization. The apparent molecular weight determined by gel filtration was 215,000 卤 20,000...