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Pregled bibliografske jedinice broj: 686500

Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor.

Mu, Linjing; Bieri, Daniel; Slavik, Roger; Drandarov, Konstantin; Müller, Adrienne; Čermak, Stjepko; Weber, Markus; Krämer, Stefanie D.; Schibli, Roger; Ametamey, Simon M.;
Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor. // Journal of neurochemistry, 126 (2013), 5; 616-624 doi:10.1111/jnc.12354 (međunarodna recenzija, članak, znanstveni)

CROSBI ID: 686500 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor.

Autori
Mu, Linjing ; Bieri, Daniel ; Slavik, Roger ; Drandarov, Konstantin ; Müller, Adrienne ; Čermak, Stjepko ; Weber, Markus ; Krämer, Stefanie D. ; Schibli, Roger ; Ametamey, Simon M. ;

Izvornik
Journal of neurochemistry (0022-3042) 126 (2013), 5; 616-624

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
autoradiography; cannabinoid receptor type 2 ligand; neurodegeneration; radiolabeling; small-animal PET

Sažetak
The cannabinoid type 2 (CB2) receptor plays an important role in neuroinflammatory and neurodegenerative diseases such as multiple sclerosis, amyotrophic lateral sclerosis, and Alzheimer’s disease and is therefore a very promising target for therapeutic approaches as well as for imaging. Based on the literature, we identified one 4-oxoquinoline derivative(designated KD2) as the lead structure. It was synthesized, radiolabeled and evaluated as a potential imaging tracer for CB2. [11C]KD2 was obtained in 99% radiochemical purity.Moderate blood–brain barrier (BBB) passage was predicted for KD2 from an in vitro transport assay with P- glycoprotein-transfected Madin Darby canine kidney cells. No efflux of KD2 by P-glycoprotein was detected. In vitro autoradiography of rat and mouse spleen slices demonstrated that [11C]KD2 exhibits high specific binding towards CB2. High spleen uptake of [11C]KD2 was observed in dynamic positron emission tomography(PET) studies with Wistar rats and its specificity was confirmed by displacement study with a selective CB2 agonist, GW405833. A pilot autoradiography study with post- mortem spinal cord slices from amyotrophic lateral sclerosis (ALS)patients with [11C]KD2 suggested the presence of CB2 receptors under disease conditions. Specificity of [11C]KD2 binding could also be demonstrated on these human tissues. In conclusion, [11C]KD2 shows good in vitro and in vivo properties as a potential PET tracer for CB2.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA

Ustanove:
Institut "Ruđer Bošković", Zagreb

Profili:

Avatar Url Stjepko Čermak (autor)

Poveznice na cjeloviti tekst rada:

doi onlinelibrary.wiley.com www.ncbi.nlm.nih.gov

Citiraj ovu publikaciju:

Mu, Linjing; Bieri, Daniel; Slavik, Roger; Drandarov, Konstantin; Müller, Adrienne; Čermak, Stjepko; Weber, Markus; Krämer, Stefanie D.; Schibli, Roger; Ametamey, Simon M.;
Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor. // Journal of neurochemistry, 126 (2013), 5; 616-624 doi:10.1111/jnc.12354 (međunarodna recenzija, članak, znanstveni)
Mu, L., Bieri, D., Slavik, R., Drandarov, K., Müller, A., Čermak, S., Weber, M., Krämer, S., Schibli, R., Ametamey, S. & (2013) Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor.. Journal of neurochemistry, 126 (5), 616-624 doi:10.1111/jnc.12354.
@article{article, author = {Mu, Linjing and Bieri, Daniel and Slavik, Roger and Drandarov, Konstantin and M\"{u}ller, Adrienne and \v{C}ermak, Stjepko and Weber, Markus and Kr\"{a}mer, Stefanie D. and Schibli, Roger and Ametamey, Simon M.}, year = {2013}, pages = {616-624}, DOI = {10.1111/jnc.12354}, keywords = {autoradiography, cannabinoid receptor type 2 ligand, neurodegeneration, radiolabeling, small-animal PET}, journal = {Journal of neurochemistry}, doi = {10.1111/jnc.12354}, volume = {126}, number = {5}, issn = {0022-3042}, title = {Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor.}, keyword = {autoradiography, cannabinoid receptor type 2 ligand, neurodegeneration, radiolabeling, small-animal PET} }
@article{article, author = {Mu, Linjing and Bieri, Daniel and Slavik, Roger and Drandarov, Konstantin and M\"{u}ller, Adrienne and \v{C}ermak, Stjepko and Weber, Markus and Kr\"{a}mer, Stefanie D. and Schibli, Roger and Ametamey, Simon M.}, year = {2013}, pages = {616-624}, DOI = {10.1111/jnc.12354}, keywords = {autoradiography, cannabinoid receptor type 2 ligand, neurodegeneration, radiolabeling, small-animal PET}, journal = {Journal of neurochemistry}, doi = {10.1111/jnc.12354}, volume = {126}, number = {5}, issn = {0022-3042}, title = {Radiolabeling and in vitro /in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1, 4- dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor.}, keyword = {autoradiography, cannabinoid receptor type 2 ligand, neurodegeneration, radiolabeling, small-animal PET} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE

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