KOBV Portal

Hits per page

hits 1 - 8 | 8 hits

Sorting

Online Resource

Development and Evaluation of Novel PET Tracers for Imaging Cannabinoid Receptor Type 2 in Brain

Slavik, Roger ; Bieri, Daniel ; Čermak, Stjepko ; [et al.]

Swiss Chemical Society ; 2014

In: CHIMIA Vol. 68, No. 4 ( 2014-04-30), p. 208-

add to watchlist on the watchlist

Details

In: CHIMIA, Swiss Chemical Society, Vol. 68, No. 4 ( 2014-04-30), p. 208-

Abstract: The cannabinoid receptor type 2 (CB2) has a very low expression level in brain tissue under basal conditions, but it is up-regulated in diverse pathological conditions. Two promising lead structures from the literature, N-((3S,5S,7S)-adamantan-1-yl)-8-methoxy-4-oxo-1-pentyl-1,4-dihydroquinoline-3-carboxamide and 8-butoxy-N-(2-fluoro-2-phenylethyl)-7-methoxy-2-oxo-1,2-dihydroquinoline-3-carboxamide – designated KD2 and KP23, respectively – were evaluated as potential PET ligands for imaging CB2. Both KD2 and KP23 were synthesized and labeled with carbon-11. In vitro autoradiographic studies on rodent spleen tissues showed that [11C]KD2 exhibits superior properties. A pilot study using [11C] KD2 on human post mortem ALS spinal cord slices indicated high CB2 expression level and specific binding, a very exciting finding if considering the future diagnostic application of CB2 ligands and their utility in therapy monitoring. In vivo blocking studies in rats with [11C] KD2 showed also high specific uptake in spleen tissue. Although the protein-bound fraction is relatively high, KD2 or KD2 derivatives could be very useful tools for the non-invasive investigation of CB2 levels under various neuroinflammatory conditions.

Type of Medium: Online Resource

ISSN: 2673-2424 , 0009-4293

URL: Article

DOI: 10.2533/chimia.2014.208

RVK:

VA 3600

Language: Unknown

Publisher: Swiss Chemical Society

Publication Date: 2014

detail.hit.zdb_id: 2179192-2

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

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 ; [et al.]

Wiley ; 2013

In: Journal of Neurochemistry Vol. 126, No. 5 ( 2013-09), p. 616-624

add to watchlist on the watchlist

Details

In: Journal of Neurochemistry, Wiley, Vol. 126, No. 5 ( 2013-09), p. 616-624

Abstract: The cannabinoid type 2 (CB 2 ) 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 KD 2) as the lead structure. It was synthesized, radiolabeled and evaluated as a potential imaging tracer for CB 2 . [ 11 C] KD 2 was obtained in 99% radiochemical purity. Moderate blood–brain barrier ( BBB ) passage was predicted for KD 2 from an in vitro transport assay with P‐glycoprotein‐transfected Madin Darby canine kidney cells. No efflux of KD 2 by P‐glycoprotein was detected. In vitro autoradiography of rat and mouse spleen slices demonstrated that [ 11 C] KD 2 exhibits high specific binding towards CB 2 . High spleen uptake of [ 11 C] KD 2 was observed in dynamic positron emission tomography (PET) studies with Wistar rats and its specificity was confirmed by displacement study with a selective CB 2 agonist, GW 405833. A pilot autoradiography study with post‐mortem spinal cord slices from amyotrophic lateral sclerosis ( ALS ) patients with [ 11 C] KD 2 suggested the presence of CB 2 receptors under disease conditions. Specificity of [ 11 C] KD 2 binding could also be demonstrated on these human tissues. In conclusion, [ 11 C] KD 2 shows good in vitro and in vivo properties as a potential PET tracer for CB 2 . image The cannabinoid type 2 receptor (CB 2 ) plays an important role in neuroinflammatory and neuro–degenerative diseases. [ 11 C]KD2, a new CB 2 radioligand, exhibits selectivity towards CB 2 receptor in vitro and in vivo in rat. A pilot autoradiography study with spinal cord slices from amyotrophic lateral sclerosis patients with [ 11 C]KD2 suggested the presence of CB 2 under disease conditions (Figure). Selective CB 2 agonist, GW405833.

Type of Medium: Online Resource

ISSN: 0022-3042 , 1471-4159

URL: Issue

URL: Article

DOI: 10.1111/jnc.2013.126.issue-5

DOI: 10.1111/jnc.12354

Language: English

Publisher: Wiley

Publication Date: 2013

detail.hit.zdb_id: 2020528-4

SSG: 12

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

Synthesis and Biological Evaluation of Quinoxaline Derivatives for PET Imaging of the NMDA Receptor

Milicevic Sephton, Selena ; Vetterli, Peter T. ; Pedani, Valentina ; [et al.]

Wiley ; 2017

In: Helvetica Chimica Acta Vol. 100, No. 12 ( 2017-12)

add to watchlist on the watchlist

Details

In: Helvetica Chimica Acta, Wiley, Vol. 100, No. 12 ( 2017-12)

Abstract: Due to the biological complexity of the N ‐methyl‐ d ‐aspartate receptor ( NMDAR ), the development of a positron emission tomography radiotracer for the imaging of NMDAR has met with limited success. Recent studies have established the presence of GluN2A subunit of the NMDAR in the heart and its role in the regulation of intracellular calcium levels. In our efforts to develop an imaging agent for the GluN2A subunit, we designed three new compounds based on a quinoxaline scaffold. The synthesis of the analogues was based on a two‐step Kabachnik–Fields reaction in sequence with Suzuki cross‐coupling and acid hydrolysis. They exhibited comparable high binding affinity values below 5 n m . A two‐step radiolabeling procedure was successfully developed for the synthesis of [ 18 F] 1 . [ 18 F] 1 was obtained in a modest overall radiochemical yield of 5.5 ± 4.2%, a good specific radioactivity of 254 ± 158 GBq/μmol, and a radiochemical purity 〉 99%. While compounds 2 and 3 showed comparable binding affinity towards NMDAR , sluggish radiolabeling, prevented their further evaluation. For [ 18 F] 1 , in vitro autoradiography on rat heart slices demonstrated heterogeneous but unspecific accumulation, whereas for the brain a high in vitro specificity towards NMDAR , could be demonstrated.

Type of Medium: Online Resource

ISSN: 0018-019X , 1522-2675

URL: Issue

URL: Article

DOI: 10.1002/hlca.v100.12

DOI: 10.1002/hlca.201700204

RVK:

VA 4500

Language: English

Publisher: Wiley

Publication Date: 2017

detail.hit.zdb_id: 74-7

detail.hit.zdb_id: 1475013-2

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

Loss of Cathepsin B and L Leads to Lysosomal Dysfunction, NPC-Like Cholesterol Sequestration and Accumulation of the Key Alzheimer's Proteins

Cermak, Stjepko ; Kosicek, Marko ; Mladenovic-Djordjevic, Aleksandra ; [et al.]

Public Library of Science (PLoS) ; 2016

In: PLOS ONE Vol. 11, No. 11 ( 2016-11-30), p. e0167428-

add to watchlist on the watchlist

Details

In: PLOS ONE, Public Library of Science (PLoS), Vol. 11, No. 11 ( 2016-11-30), p. e0167428-

Type of Medium: Online Resource

ISSN: 1932-6203

URL: Article

DOI: 10.1371/journal.pone.0167428

DOI: 10.1371/journal.pone.0167428.g001

DOI: 10.1371/journal.pone.0167428.g002

DOI: 10.1371/journal.pone.0167428.g003

DOI: 10.1371/journal.pone.0167428.g004

DOI: 10.1371/journal.pone.0167428.g005

DOI: 10.1371/journal.pone.0167428.g006

DOI: 10.1371/journal.pone.0167428.s001

DOI: 10.1371/journal.pone.0167428.s002

DOI: 10.1371/journal.pone.0167428.s003

Language: English

Publisher: Public Library of Science (PLoS)

Publication Date: 2016

detail.hit.zdb_id: 2267670-3

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

P4‐251: ALTERED METABOLISM OF BACE1 SUBSTRATES SEIZURE PROTEIN 6 AND SEIZURE 6‐LIKE PROTEIN 1 IN NIEMANN‐PICK TYPE C DISEASE

Cermak, Stjepko ; Causevic, Mirsada ; Kuhn, Peer‐Hendrik ; [et al.]

Wiley ; 2014

In: Alzheimer's & Dementia Vol. 10, No. 4S_Part_15 ( 2014-07)

add to watchlist on the watchlist

Details

In: Alzheimer's & Dementia, Wiley, Vol. 10, No. 4S_Part_15 ( 2014-07)

Type of Medium: Online Resource

ISSN: 1552-5260 , 1552-5279

URL: Article

DOI: 10.1016/j.jalz.2014.07.022

Language: English

Publisher: Wiley

Publication Date: 2014

detail.hit.zdb_id: 2201940-6

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

BACE1-cleavage of Sez6 and Sez6L is elevated in Niemann-Pick type C disease mouse brains

Causevic, Mirsada ; Dominko, Kristina ; Malnar, Martina ; [et al.]

Public Library of Science (PLoS) ; 2018

In: PLOS ONE Vol. 13, No. 7 ( 2018-7-6), p. e0200344-

add to watchlist on the watchlist

Details

In: PLOS ONE, Public Library of Science (PLoS), Vol. 13, No. 7 ( 2018-7-6), p. e0200344-

Type of Medium: Online Resource

ISSN: 1932-6203

URL: Article

DOI: 10.1371/journal.pone.0200344

DOI: 10.1371/journal.pone.0200344.g001

DOI: 10.1371/journal.pone.0200344.g002

DOI: 10.1371/journal.pone.0200344.g003

DOI: 10.1371/journal.pone.0200344.g004

DOI: 10.1371/journal.pone.0200344.g005

DOI: 10.1371/journal.pone.0200344.g006

DOI: 10.1371/journal.pone.0200344.g007

DOI: 10.1371/journal.pone.0200344.g008

DOI: 10.1371/journal.pone.0200344.g009

DOI: 10.1371/journal.pone.0200344.g010

DOI: 10.1371/journal.pone.0200344.s001

DOI: 10.1371/journal.pone.0200344.s002

DOI: 10.1371/journal.pone.0200344.s003

DOI: 10.1371/journal.pone.0200344.s004

DOI: 10.1371/journal.pone.0200344.s005

DOI: 10.1371/journal.pone.0200344.s006

Language: English

Publisher: Public Library of Science (PLoS)

Publication Date: 2018

detail.hit.zdb_id: 2267670-3

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

Synthesis and Preliminary Evaluation of a 2-Oxoquinoline Carboxylic Acid Derivative for PET Imaging the Cannabinoid Type 2 Receptor

Mu, Linjing ; Slavik, Roger ; Müller, Adrienne ; [et al.]

MDPI AG ; 2014

In: Pharmaceuticals Vol. 7, No. 3 ( 2014-03-06), p. 339-352

add to watchlist on the watchlist

Details

In: Pharmaceuticals, MDPI AG, Vol. 7, No. 3 ( 2014-03-06), p. 339-352

Type of Medium: Online Resource

ISSN: 1424-8247

URL: Article

DOI: 10.3390/ph7030339

Language: English

Publisher: MDPI AG

Publication Date: 2014

detail.hit.zdb_id: 2193542-7

SSG: 15,3

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

Online Resource

Synthesis and Biological Evaluation of a New Acyclic Pyrimidine Derivative as a Probe for Imaging Herpes Simplex Virus Type 1 Thymidine Kinase Gene Expression

Meščić, Andrijana ; Betzel, Thomas ; Müller, Adrienne ; [et al.]

MDPI AG ; 2013

In: Molecules Vol. 18, No. 7 ( 2013-07-19), p. 8535-8549

add to watchlist on the watchlist

Details

In: Molecules, MDPI AG, Vol. 18, No. 7 ( 2013-07-19), p. 8535-8549

Type of Medium: Online Resource

ISSN: 1420-3049

URL: Article

DOI: 10.3390/molecules18078535

Language: English

Publisher: MDPI AG

Publication Date: 2013

detail.hit.zdb_id: 2008644-1

Bookmarklink

Library	Location	Call Number	Volume/Issue/Year	Availability

Others were also interested in ...

Online Resource

Open Access Request

Availability (electronic / print)

Link to publisher

hits 1 - 8 | 8 hits

Nothing or not found what you are looking for? Please check your search query or use the Interlibrary Loan Search.

Kooperativer Bibliotheksverbund

Berlin Brandenburg