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Chemical Compound Review:

CHEMBL1817977 N-butan-2-yl-1-(2- chlorophenyl)-N-methyl...

Synonyms: MOLI001365, AC1L9P7B, PK-11195 C-11, [11C]PK11195, 124236-60-8, ...

Pappata, S. et al., Versijpt, J. et al., Cumming, P. et al., Gerhard, A. et al., Debruyne, J.C. et al., et al.

Debruyne, Versijpt, Van Laere, De Vos, Keppens, Strijckmans, Achten, Slegers, Dierckx, Korf, De Reuck, Pappata, Levasseur, Gunn, Myers, Crouzel, Syrota, Jones, Kreutzberg, Banati, Debruyne, Van Laere, Versijpt, De Vos, Eng, Strijckmans, Santens, Achten, Slegers, Korf, Dierckx, De Reuck, Cumming, Pedersen, Minuzzi, Mezzomo, Danielsen, Iversen, Aagaard, Keiding, Munk, Finsen,

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Disease relevance of MOLI001365

OBJECTIVE: The objectives of the present study were to assess brain atrophy in multiple sclerosis (MS) patients during different disease stages and to investigate by PET and [11C]PK11195, a marker of microglial activation, the relationship between inflammation, atrophy and clinically relevant measures [1].
To investigate the microglial reaction in stroke we used a marker for activated microglia, [11C]PK11195, and PET in five patients with ischemic stroke 5-53 days after infarction [2].

High impact information on MOLI001365

Using quantitative PET, the authors studied the binding of [11C]PK11195, a marker of activated microglia, in the thalamus of patients with chronic middle cerebral artery infarcts [3].
[11C]PK11195, a selective PBR antagonist, has been used for the in vivo PET monitoring of neurodegeneration in clinical observations [4].
The cerebral distribution of peripheral-type benzodiazepine binding sites (PBBS) in human brain has been investigated by positron emission tomography (PET) with the specific radioligand [11C]PK11195 in diverse neuropathological conditions [5].
The positron emission tomography ligand [11C]PK11195 may be useful for the assessment of thiamine deficiency-induced brain damage in human alcoholics [6].
PET visualization of microglia in multiple sclerosis patients using [11C]PK11195 [7].

Chemical compound and disease context of MOLI001365

Semiquantification of the peripheral-type benzodiazepine ligand [11C]PK11195 in normal human brain and application in multiple sclerosis patients [8].

Anatomical context of MOLI001365

All patients showed increased [11C]PK11195 binding in the ipsilateral thalamus, indicating the activation of microglia in degenerating projection areas remote from the primary lesion [3].

Gene context of MOLI001365

[11C]PK11195 is a positron emission tomography (PET) radioligand for the PBR [7].

Analytical, diagnostic and therapeutic context of MOLI001365

Positron emission tomography (PET) using [11C]PK11195 could offer a potentially useful diagnostic tool in WKS in humans [9].

References

Microglial imaging with positron emission tomography and atrophy measurements with magnetic resonance imaging in multiple sclerosis: a correlative study. Versijpt, J., Debruyne, J.C., Van Laere, K.J., De Vos, F., Keppens, J., Strijckmans, K., Achten, E., Slegers, G., Dierckx, R.A., Korf, J., De Reuck, J.L. Mult. Scler. (2005) [Pubmed]
In vivo imaging of activated microglia using [11C]PK11195 and positron emission tomography in patients after ischemic stroke. Gerhard, A., Neumaier, B., Elitok, E., Glatting, G., Ries, V., Tomczak, R., Ludolph, A.C., Reske, S.N. Neuroreport (2000) [Pubmed]
Thalamic microglial activation in ischemic stroke detected in vivo by PET and [11C]PK1195. Pappata, S., Levasseur, M., Gunn, R.N., Myers, R., Crouzel, C., Syrota, A., Jones, T., Kreutzberg, G.W., Banati, R.B. Neurology (2000) [Pubmed]
Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration. Belloli, S., Moresco, R.M., Matarrese, M., Biella, G., Sanvito, F., Simonelli, P., Turolla, E., Olivieri, S., Cappelli, A., Vomero, S., Galli-Kienle, M., Fazio, F. Neurochem. Int. (2004) [Pubmed]
Distribution of PK11195 binding sites in porcine brain studied by autoradiography in vitro and by positron emission tomography. Cumming, P., Pedersen, M.D., Minuzzi, L., Mezzomo, K., Danielsen, E.H., Iversen, P., Aagaard, D., Keiding, S., Munk, O.L., Finsen, B. Synapse (2006) [Pubmed]
Quantitative autoradiography using selective radioligands for central and peripheral-type benzodiazepine receptors in experimental Wernicke's encephalopathy: implications for positron emission tomography imaging. Leong, D.K., Oliva, L., Butterworth, R.F. Alcohol. Clin. Exp. Res. (1996) [Pubmed]
PET visualization of microglia in multiple sclerosis patients using [11C]PK11195. Debruyne, J.C., Versijpt, J., Van Laere, K.J., De Vos, F., Keppens, J., Strijckmans, K., Achten, E., Slegers, G., Dierckx, R.A., Korf, J., De Reuck, J.L. Eur. J. Neurol. (2003) [Pubmed]
Semiquantification of the peripheral-type benzodiazepine ligand [11C]PK11195 in normal human brain and application in multiple sclerosis patients. Debruyne, J.C., Van Laere, K.J., Versijpt, J., De Vos, F., Eng, J.K., Strijckmans, K., Santens, P., Achten, E., Slegers, G., Korf, J., Dierckx, R.A., De Reuck, J.L. Acta neurologica Belgica. (2002) [Pubmed]
Increased densities of binding sites for the "peripheral-type" benzodiazepine receptor ligand [3H]PK11195 in vulnerable regions of the rat brain in thiamine deficiency encephalopathy. Leong, D.K., Le, O., Oliva, L., Butterworth, R.F. J. Cereb. Blood Flow Metab. (1994) [Pubmed]

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