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Publikasjoner
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Bow, John-Paul J. & Riss, Patrick Johannes
(2021).
Phosgene-Free Carbonyl Insertion: Hot Advances in <sup>11</sup>C-Chemistry.
Chemistry-Methods.
ISSN 2628-9725.
1(3),
s. 139–141.
doi:
10.1002/cmtd.202000029.
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Perez Garcia, Raul Manuel; Grønnevik, Gaute & Riss, Patrick
(2021).
A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates.
Organic Letters.
ISSN 1523-7060.
23(3),
s. 1011–1015.
doi:
10.1021/acs.orglett.0c04209.
Fulltekst i vitenarkiv
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Gurin, Andrey; Chakrova, Yelena; Matveyeva, Ilona & Riss, Patrick Johannes
(2020).
Optimization of reaction parameters for the synthesis of 177Lu-DOTAELA.
Revista de chimie (Bucuresti).
ISSN 0034-7752.
71(8),
s. 55–62.
doi:
10.37358/RC.20.8.8278.
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Gurin, A.N.; Riss, Patrick; Chakrova, E.T.; Matveyeva, I.V. & Kadyrbaev, E.A.
(2020).
Study of the Purification of <sup>177</sup>Lu-DOTAELA Complex.
Pharmaceutical Chemistry Journal.
ISSN 0091-150X.
54(1),
s. 64–68.
doi:
10.1007/s11094-020-02157-3.
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Jakobsson, Jimmy Erik; Gourni, Eleni; Shivashankar, Shivashankar; Brito, Beatriz & Riss, Patrick
(2019).
Synthesis and Characterization in Rodent Brain of the Subtype-Selective NR2B NMDA Receptor Ligand [11C]Ro04-5595 as a Potential Radiotracer for Positron Emission Tomography.
ACS Omega.
ISSN 2470-1343.
4(6),
s. 9925–9931.
doi:
10.1021/acsomega.9b00357.
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Jakobsson, Jimmy Erik; Grønnevik, Gaute; Rafique, Waqas; Hartvig, Karoline & Riss, Patrick
(2018).
Formamide as an Unconventional Amine Protecting Group for PET Radiochemistry.
European Journal of Organic Chemistry.
ISSN 1434-193X.
2018(27),
s. 3701–3704.
doi:
10.1002/ejoc.201800554.
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Jakobsson, Jimmy Erik & Riss, Patrick
(2018).
Transition metal free, late-stage, regiospecific, aromatic fluorination on a preparative scale using a KF/crypt-222 complex.
RSC Advances.
ISSN 2046-2069.
8(38),
s. 21288–21291.
doi:
10.1039/c8ra03757d.
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Alluri, Santosh Reddy & Riss, Patrick
(2018).
Stereospecific radiosynthesis of 3-fluoro amino acids: access to enantiomerically pure radioligands for positron emission tomography.
Organic and biomolecular chemistry.
ISSN 1477-0520.
16(13),
s. 2219–2224.
doi:
10.1039/c8ob00184g.
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Fjellaksel, Richard; Sundset, Rune; Riss, Patrick & Hansen, Jørn H
(2018).
Copper-mediated late-stage iodination and 123I-labelling of
triazole-benzimidazole bioactives.
Synlett : Accounts and Rapid Communications in Synthetic Organic Chemistry.
ISSN 0936-5214.
29(11),
s. 1491–1495.
doi:
10.1055/s-0036-1591985.
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Jakobsson, Jimmy Erik; Grønnevik, Gaute & Riss, Patrick
(2017).
Organocatalyst-assisted Ar-18F bond formation: A universal procedure for direct aromatic radiofluorination.
Chemical Communications.
ISSN 1359-7345.
53(96),
s. 12906–12909.
doi:
10.1039/c7cc07211b.
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Rafique, Waqas; Shivashankar, Shivashankar; Milde, Mona & Riss, Patrick
(2017).
Reaching out for sensitive evaluation of the Mu opioid receptor in vivo: positron emission tomography imaging of the Agonist [11C]AH7921.
ACS Chemical Neuroscience.
ISSN 1948-7193.
8(9),
s. 1847–1852.
doi:
10.1021/acschemneuro.7b00075.
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Fjellaksel, Richard; Boomgaren, Marc; Sundset, Rune; Haraldsen, Ira Hebold; Hansen, Jørn H & Riss, Patrick
(2017).
Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor.
MedChemComm.
ISSN 2040-2503.
8(10),
s. 1965–1969.
doi:
10.1039/c7md00320j.
Fulltekst i vitenarkiv
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Maschauer, Simone; Haller, Adelina; Riss, Patrick; Kuwert, Torsten; Prante, Olaf & Cumming, Paul
(2015).
Specific binding of [18F]fluoroethyl-harmol to monoamine oxidase A in rat brain cryostat sections, and compartmental analysis of binding in living brain.
Journal of Neurochemistry.
ISSN 0022-3042.
135(5),
s. 908–917.
doi:
10.1111/jnc.13370.
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Cumming, Paul; Maschauer, Simone; Riss, Patrick; Grill, Eva; Pischetsrieder, Monika & Kuwert, Torsten
[Vis alle 7 forfattere av denne artikkelen]
(2015).
Perturbed Development of Striatal Dopamine Transporters in Fatty Versus Lean Zucker Rats: a Follow-up Small Animal PET Study.
Molecular Imaging and Biology.
ISSN 1536-1632.
17(4),
s. 521–528.
doi:
10.1007/s11307-014-0811-7.
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Cumming, Paul; Maschauer, Simone; Riss, Patrick; Tschammer, Nuska; Fehler, Stefanie K. & Heinrich, Markus R.
[Vis alle 8 forfattere av denne artikkelen]
(2014).
Radiosynthesis and validation of 18 F-FP-CMT, a phenyltropane with superior properties for imaging the dopamine transporter in living brain.
Journal of Cerebral Blood Flow and Metabolism.
ISSN 0271-678X.
34(7),
s. 1148–1156.
doi:
10.1038/jcbfm.2014.63.
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Rühl, Thomas; Rafique, Waqas; Lien, Vegard Torp & Riss, Patrick
(2014).
Cu(I)-mediated 18F-trifluoromethylation of arenes: Rapid synthesis of 18F-labeled trifluoromethyl arenes†.
Chemical Communications.
ISSN 1359-7345.
50(45),
s. 6056–6059.
doi:
10.1039/c4cc01641f.
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Riss, Patrick; Hong, Young T.; Marton, Janos; Caprioli, Daniele; Williamson, Derek & Ferrari, Valentina
[Vis alle 12 forfattere av denne artikkelen]
(2013).
Synthesis and Evaluation of F-18-FE-PEO in Rodents: An F-18-Labeled Full Agonist for Opioid Receptor Imaging.
Journal of Nuclear Medicine.
ISSN 0161-5505.
54(2),
s. 299–305.
doi:
10.2967/jnumed.112.108688.
Se alle arbeider i Cristin
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Gurin, A.N.; Riss, Patrick Johannes; Chakrova, E.T.; Matveyeva, I.V. & Kadyrbaev, E.A.
(2020).
Correction to: Study of the Purification of <sup>177</sup>Lu-DOTAELA Complex (Pharmaceutical Chemistry Journal, (2020), 54, 1, (64-68), 10.1007/s11094-020-02157-3).
Pharmaceutical Chemistry Journal.
ISSN 0091-150X.
54(7).
doi:
10.1007/s11094-020-02270-3.
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Kristian, Alexandr; Riss, Patrick; Qu, Hong; Milde, Mona; Schoultz, Bent Wilhelm & Engebråten, Olav
[Vis alle 8 forfattere av denne artikkelen]
(2014).
Pharmacokinetic modeling of dynamic 18F‐Choline PET reflects choline metabolism in breast carcinoma xenografts.
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Hartvig, Karoline; Riss, Patrick; Hjelstuen, Olaug & Brevik, Ellen Mengshoel
(2020).
Synthesis and evaluation of radiopharmaceuticals for targeted radionuclide therapy.
Universitetet i Oslo.
Vis sammendrag
Nowadays, radionuclides play an important role in oncology, especially in the developing field of targeted radionuclide therapy (TRT). In this master thesis, the focus is to evaluate different radiolabeled targeting molecules for human epidermal growth factor receptor 2 (HER2) positive breast cancer and metastatic castration-resistant prostate cancer (mCRPC). The chosen targeting molecules are Herceptin® (trastuzumab) and PSMA-617, which will specifically target HER2- and PSMA-receptors, respectively. The HER2- and PSMA-receptors are excellent targets for use in targeted radionuclide therapy and should be explored further to achieve better and more efficient treatments than current treatments and for obtaining more personalized treatment regimens for patients. The β-emitter lutetium-177 (177Lu) has been thoroughly investigated with both trastuzumab and PSMA-617, but the use of the α-emitter actinium-225 (225Ac) is less studied with these targeting molecules. Although the 225Ac-PSMA-617 has been tested in patients, there is still a need for more knowledge about actinium-225, and a deeper understanding of the use of 225Ac in PSMA-617 and trastuzumab with regard to radiolabeling conditions, stability and their effects on cancer cells. This work has resulted in a successful synthesis of 225Ac-DOTA-trastuzumab, 225Ac-PSMA-617, [177Lu]Lu-DOTA-trastuzumab and [177Lu]Lu-PSMA-617 with high radiochemical yields (> 90 %). A new radiolabeling routine was obtained for 225Ac-PSMA-617 giving a yield of 98 % with good reproducibility. Furthermore, the stability of each radiolabeled conjugate has been thoroughly investigated and showed that all radiolabeled conjugates had a shelf-life of five days in the temperature range of 5-37 °C, except for 225Ac-DOTA-trastuzumab which only showed high stability over two days. Moreover, radiolysis effects were not observed for 225Ac-PSMA-617 samples with specific activities up to 216 kBq/µg, showing high stabilities over two weeks with approximately 90 % radiochemical purity. For 225Ac-DOTA-trastuzumab, only the samples with the lowest specific activities (< 1357 kBq/mg) were unaffected by radiolysis. The cell binding assays resulted in high cell-binding values of 94 % and 93 % for 225Ac-DOTA-trastuzumab and [177Lu]Lu-DOTA-trastuzumab on SKBR-3 cells. Furthermore, cell-binding values of 84 % and 85 % were obtained for 225Ac-PSMA-617 and [177Lu]Lu-PSMA-617 on LNCaP cells. Cell viability assays were performed and showed that 225Ac-PSMA-617 (in the range 2.5-600 Bq) is a more efficient therapeutic agent than [177Lu]Lu-PSMA-617 (in the range 50-400 kBq). The cell viability assays also confirmed that 225Ac-DOTA-trastuzumab has the potential of being a more efficient agent for the treatment of HER2-positive breast cancer than non-radioactive Herceptin®. The results of this thesis provide a significant contribution to the field of targeted alpha therapy (TAT) through studying the radiolabeling with 225Ac, the stability of 225Ac-labeled conjugates, their binding affinities and their ability to deplete cancer cells of ATP.
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Rafique, Waqas; Riss, Patrick & Omtvedt, Jon Petter
(2018).
Synthesis of Fluorine-18 Labelled Radiotraces and Their Pre-Clinical and Clinical Characterization.
Kjemisk institutt, Universitetet i Oslo.
ISSN 1501-7710.
2018(2013).
Vis sammendrag
Positron emission tomography (PET) is one of the most sensitive in vivo imaging techniques available to clinicians and researchers. It helps in understanding the biological interactions and mechanism of various diseases through use of radiolabelled compounds called radiotracers.
Herein is described the development of facile radiolabelling approaches for straightforward access to 18F-labelled trifluoromethyl radiotracers. Direct nucleophilic radiofluorination of difluorovinyl precursors was achieved for 18F-trifluoromethylation of aliphatic compounds, and applied to the radiosynthesis of [18F]lansoprazole and N-methyl[18F]lansoprazole. The compounds were used to analyze the blood-brain barrier penetration in healthy persons and for the detection of tau-neurofibrillary tangles in Alzheimer’s patients.
For 18F-trifluoromethylation of aromatic compounds, in situ synthesis of Cu[18F]CF3 was achieved and used in 18F-trifluoromethylation of iodo-arenes using a single vial one-step method. The procedure was applied for radiosynthesis of a derivative of AH7921, which is a sub-type selective mu-opioid receptor agonist. The developed procedures are applicable to available radiosynthesis hardware, and provide access to desired compounds within 40 minutes in high radiochemical yields.
In addition, a series of new compounds were synthesized with aim to discover the new radioligands based on modifications to the lead compounds i.e. lansoprazole and AH7921. Several interesting candidates with good combination of affinity and selectivity were identified from each series, and radiolabelled with fluorine-18. The newly developed 18F-labelled compounds have good potential to provide the in vivo characterization of tau-neurofibrillary tangles and quantification of the opioid receptors using the PET imaging.
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Publisert
18. juni 2018 12:36
- Sist endret
20. okt. 2020 10:30