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2. Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates

Author

Arakawa, Ryosuke, Takano, Akihiro, Nag, Sangram, Jia, Zhisheng, Amini, Nahid, Maresca, Kevin P., Zhang, Lei, Keliher, Edmund J., Butler, Christopher R., Piro, Justin R., Samad, Tarek A., Smith, Deborah, Nason, Deane, O’Neil, Steve, Trapa, Patrick, Fonseca, Kari R., Litchfield, John, McCarthy, Timothy, Carson, Richard E., and Halldin, Christer

Published
2022
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7. Synthesis of [11C]BIIB104, an α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic-Acid-Positive Allosteric Modulator, and Evaluation of the Bio-Distribution in Non-Human Primate Brains Using Positron Emission Tomography

Author

Nag, Sangram, primary, Jia, Kevin, additional, Arakawa, Ryosuke, additional, Datta, Prodip, additional, Scott, Daniel, additional, Shaffer, Christopher, additional, Moein, Mohammad Mahdi, additional, Hutchison, Matthew, additional, Kaliszczak, Maciej, additional, and Halldin, Christer, additional

Published
2024
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13. Development of a Novel [11C]CO-Labeled Positron Emission Tomography Radioligand [11C]BIO-1819578 for the Detection of O-GlcNAcase Enzyme Activity

Author

Nag, Sangram, primary, Bolin, Martin, additional, Datta, Prodip, additional, Arakawa, Ryosuke, additional, Forsberg Morén, Anton, additional, Khani Maynaq, Yasir, additional, Lin, Edward, additional, Genung, Nathan, additional, Hering, Heike, additional, Guckian, Kevin, additional, Martarello, Laurent, additional, Kaliszczak, Maciej, additional, and Halldin, Christer, additional

Published
2023
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15. Synthesis of [ 11 C]BIIB104, an α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic-Acid-Positive Allosteric Modulator, and Evaluation of the Bio-Distribution in Non-Human Primate Brains Using Positron Emission Tomography.

Author

Nag, Sangram, Jia, Kevin, Arakawa, Ryosuke, Datta, Prodip, Scott, Daniel, Shaffer, Christopher, Moein, Mohammad Mahdi, Hutchison, Matthew, Kaliszczak, Maciej, and Halldin, Christer

Subjects
POSITRON emission tomography, GLUTAMATE receptors, RADIOCHEMICAL purification, AMPA receptors, PRIMATES
Abstract

The aim of this study was to measure the brain penetrance and kinetics of BIIB104, a first-in-class AMPA receptor potentiator developed for cognitive impairment associated with schizophrenia. It was recently halted in phase 2 clinical development, and there are a lack of tools to directly measure AMPA receptor engagement. To achieve this, the drug candidate was radiolabeled with carbon-11, and its brain penetrance and kinetics were measured in non-human primates via dynamic PET scans. Radiolabeling was achieved through a three-step nucleophilic [11C]cyanation reaction in one pot, resulting in the high radioactivity and radiochemical purity (>99%) of [11C]BIIB104. The study found that [11C]BIIB104 entered the non-human primate brains at 4–5% ID at peak, with a homogeneous distribution. However, a mild regional heterogeneity was observed in the thalamus. The lack of conclusive evidence for a change in regional values after BIIB104 dosing suggests that any specific binding component of BIIB104 is negligible compared to the free and non-specific components in the living brain. Overall, the study demonstrated high brain uptake with minor variability in [11C]BIIB104 distribution across various brain regions, its kinetics were consistent with those of passive diffusion, and the dominating components were the free concentration and non-specific binding. This information is valuable for understanding the potential effects and mechanisms of BIIB104 in the brain. [ABSTRACT FROM AUTHOR]

Published
2024
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19. Supplementary Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs

Author

Colclough, Nicola, primary, Chen, Kan, primary, Johnström, Peter, primary, Strittmatter, Nicole, primary, Yan, Yumei, primary, Wrigley, Gail L., primary, Schou, Magnus, primary, Goodwin, Richard, primary, Varnäs, Katarina, primary, Adua, Sally J., primary, Zhao, Minghui, primary, Nguyen, Don X., primary, Maglennon, Gareth, primary, Barton, Peter, primary, Atkinson, James, primary, Zhang, Lin, primary, Janefeldt, Annika, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Takano, Akihiro, primary, Arakawa, Ryosuke, primary, Kondrashov, Mikhail, primary, Malmquist, Jonas, primary, Revunov, Evgeny, primary, Vazquez-Romero, Ana, primary, Moein, Mohammad Mahdi, primary, Windhorst, Albert D., primary, Karp, Natasha A., primary, Finlay, M. Raymond V., primary, Ward, Richard A., primary, Yates, James W.T., primary, Smith, Paul D., primary, Farde, Lars, primary, Cheng, Zack, primary, and Cross, Darren A.E., primary

Published
2023
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20. Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs

Author

Colclough, Nicola, primary, Chen, Kan, primary, Johnström, Peter, primary, Strittmatter, Nicole, primary, Yan, Yumei, primary, Wrigley, Gail L., primary, Schou, Magnus, primary, Goodwin, Richard, primary, Varnäs, Katarina, primary, Adua, Sally J., primary, Zhao, Minghui, primary, Nguyen, Don X., primary, Maglennon, Gareth, primary, Barton, Peter, primary, Atkinson, James, primary, Zhang, Lin, primary, Janefeldt, Annika, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Takano, Akihiro, primary, Arakawa, Ryosuke, primary, Kondrashov, Mikhail, primary, Malmquist, Jonas, primary, Revunov, Evgeny, primary, Vazquez-Romero, Ana, primary, Moein, Mohammad Mahdi, primary, Windhorst, Albert D., primary, Karp, Natasha A., primary, Finlay, M. Raymond V., primary, Ward, Richard A., primary, Yates, James W.T., primary, Smith, Paul D., primary, Farde, Lars, primary, Cheng, Zack, primary, and Cross, Darren A.E., primary

Published
2023
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27. Correction to “Development of 11C-Labeled ASEM Analogues for Detection of Neuronal Nicotinic Acetylcholine Receptors (α7-nAChR)”

Author

Nag, Sangram, primary, Miranda-Azpiazu, Patricia, additional, Jia, Zhisheng, additional, Datta, Prodip, additional, Arakawa, Ryosuke, additional, Moein, Mohammad, additional, Yang, Zhou, additional, Tu, Yaoquan, additional, Lemoine, Laetitia, additional, Ågren, Hans, additional, Nordberg, Agneta, additional, Långström, Bengt, additional, and Halldin, Christer, additional

Published
2022
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29. Characterization of a Novel M4 PAM PET Radioligand [11C]PF06885190 in Nonhuman Primates (NHP).

Author

Nag, Sangram, Arakawa, Ryosuke, Jia, Zhisheng, Lachapelle, Erik, Zhang, Lei, Maresca, Kevin, Chen, Laigao, Jahan, Mahabuba, Mccarthy, Timothy, and Halldin, Christer

Subjects
*MUSCARINIC acetylcholine receptors, *CHOLINERGIC receptors, *KRA, *PRIMATES, *RADIOCHEMICAL purification, *ALZHEIMER'S disease
Abstract

Muscarinic acetylcholine receptors (mAChR), including M4, draw attention as therapeutic targets for several neurodegenerative diseases including Alzheimer's disease (AD). PET imaging of M4 positive allosteric modulator (PAM) allows qualification of the distribution as well as the expression of this receptor under physiological conditions and thereby helps to assess the receptor occupancy (RO) of a drug candidate. In this study, our aims were (a) to synthesize a novel M4 PAM PET radioligand [11C]PF06885190 (b) to evaluate the brain distribution of [11C]PF06885190 in nonhuman primates (NHP) and (c) to analyze its radiometabolites in the blood plasma of NHP. Radiolabeling of [11C]PF06885190 was accomplished via N-methylation of the precursor. Six PET measurements were performed using two male cynomolgus monkeys, where three PET measurements were at baseline, two after pretreatment with a selective M4 PAM compound CVL-231 and one after pretreatment with donepezil. The total volume of distribution (VT) of [11C]PF06885190 was examined using Logan graphical analysis with arterial input function. Radiometabolites were analyzed in monkey blood plasma using gradient HPLC system. Radiolabeling of [11C]PF06885190 was successfully accomplished and the radioligand was found to be stable in the formulation, with radiochemical purity exceeding 99% 1 h after the end of the synthesis. [11C]PF06885190 was characterized in the cynomolgus monkey brain where a moderate brain uptake was found at the baseline condition. However, it showed fast wash-out as it dropped to half of the peak at around 10 min. Change of VT from baseline was around −10% after pretreatment with a M4 PAM, CVL-231. Radiometabolite studies showed relatively fast metabolism. Although sufficient brain uptake of [11C]PF06885190 was observed, these data suggest that [11C]PF06885190 might have too low specific binding in the NHP brain to be further applied in PET imaging. [ABSTRACT FROM AUTHOR]

Published
2023
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30. First-in-Human Evaluation of18F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B

Author

Wakabayashi, Yuichi, primary, Stenkrona, Per, additional, Arakawa, Ryosuke, additional, Yan, Xuefeng, additional, Van Buskirk, Maia G., additional, Jenkins, Madeline D., additional, Santamaria, Jose A. Montero, additional, Maresca, Kevin P., additional, Takano, Akihiro, additional, Liow, Jeih-San, additional, Chappie, Thomas A., additional, Varrone, Andrea, additional, Nag, Sangram, additional, Zhang, Lei, additional, Hughes, Zoë A., additional, Schmidt, Christopher J., additional, Doran, Shawn D., additional, Mannes, Andrew, additional, Zanotti-Fregonara, Paolo, additional, Ooms, Maarten, additional, Morse, Cheryl L., additional, Zoghbi, Sami S., additional, Halldin, Christer, additional, Pike, Victor W., additional, and Innis, Robert B., additional

Published
2022
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32. Synthesis and biological evaluation of a novel radioligand [11C] BIO-1790735 for detection of O-GlcNAcase (OGA) enzyme activity

Author

Nag, Sangram, primary, Arakawa, Ryosuke, additional, Datta, Prodip, additional, Morén, Anton, additional, Varrone, Andrea, additional, Moein, Mohammad Mahdi, additional, Bolin, Martin, additional, Lin, Edward, additional, Genung, Nathan, additional, Martarello, Laurent, additional, Kaliszczak, Maciej, additional, and Halldin, Christer, additional

Published
2022
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33. Development of C-11-Labeled ASEM Analogues for the Detection of Neuronal Nicotinic Acetylcholine Receptors (alpha 7-nAChR)

Author

Nag, Sangram, Miranda-Azpiazu, Patricia, Jia, Zhisheng, Datta, Prodip, Arakawa, Ryosuke, Moein, Mohammad Mahdi, Zhou, Yang, Tu, Yaoquan, Lemoine, Laetitia, Ågren, Hans, Nordberg, Agneta, Långström, Bengt, Halldin, Christer, Nag, Sangram, Miranda-Azpiazu, Patricia, Jia, Zhisheng, Datta, Prodip, Arakawa, Ryosuke, Moein, Mohammad Mahdi, Zhou, Yang, Tu, Yaoquan, Lemoine, Laetitia, Ågren, Hans, Nordberg, Agneta, Långström, Bengt, and Halldin, Christer

Abstract

The homo-pentameric alpha 7 receptor is one of the major types of neuronal nicotinic acetylcholine receptors (alpha 7nAChRs) related to cognition, memory formation, and attention processing. The mapping of alpha 7-nAChRs by PET pulls a lot of attention to realize the mechanism and development of CNS diseases such as AD, PD, and schizophrenia. Several PET radioligands have been explored for the detection of the alpha 7-nAChR. F-18-ASEM is the most functional for in vivo quantification of alpha 7-nAChRs in the human brain. The first aim of this study was to initially use results from in silico and machine learning techniques to prescreen and predict the binding energy and other properties of ASEM analogues and to interpret these properties in terms of atomic structures using F-18-ASEM as a lead structure, and second, to label some selected candidates with carbon-11/hydrogen-3 (C-11/H-3) and to evaluate the binding properties in vitro and in vivo using the labeled candidates. In silico predictions are obtained from perturbation free-energy calculations preceded by molecular docking, molecular dynamics, and metadynamics simulations. Machine learning techniques have been applied for the BBB and P-gp-binding properties. Six analogues of ASEM were labeled with C-11, and three of them were additionally labeled with H-3. Binding properties were further evaluated using autoradiography (ARG) and PET measurements in non-human primates (NHPs). Radiometabolites were measured in NHP plasma. All six compounds were successfully synthesized. Evaluation with ARG showed that C-11-Kln83 was preferably binding to the alpha 7-nAChR. Competition studies showed that 80% of the total binding was displaced. Further ARG studies using H-3-KIn-83 replicated the preliminary results. In the NHP PET study, the distribution pattern of C-11-KIn-83 was similar to other alpha 7 nAChR PET tracers. The brain uptake was relatively low and increased by the administration of tariquidar, indicating a substra

Published
2022
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34. Honesty mediates the relationship between serotonin and reaction to unfairness

Author

Takahashi, Hidehiko, Takano, Harumasa, Camerer, Colin F., Ideno, Takashi, Okubo, Shigetaka, Matsui, Hiroshi, Tamari, Yuki, Takemura, Kazuhisa, Arakawa, Ryosuke, Kodaka, Fumitoshi, Yamada, Makiko, Eguchi, Yoko, Murai, Toshiya, Okubo, Yoshiro, Kato, Motoichiro, Ito, Hiroshi, and Suhara, Tetsuya

Published
2012

35. Additional file 1 of Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates

Author

Arakawa, Ryosuke, Takano, Akihiro, Nag, Sangram, Jia, Zhisheng, Amini, Nahid, Maresca, Kevin P., Zhang, Lei, Keliher, Edmund J., Butler, Christopher R., Piro, Justin R., Samad, Tarek A., Smith, Deborah, Nason, Deane, O���Neil, Steve, Trapa, Patrick, Fonseca, Kari R., Litchfield, John, McCarthy, Timothy, Carson, Richard E., and Halldin, Christer

Abstract

Additional file 1: Radioligand synthesis.

Published
2022
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37. Development of 11C-Labeled ASEM Analogues for the Detection of Neuronal Nicotinic Acetylcholine Receptors (α7-nAChR)

Author

Nag, Sangram, primary, Miranda-Azpiazu, Patricia, additional, Jia, Zhisheng, additional, Datta, Prodip, additional, Arakawa, Ryosuke, additional, Moein, Mohammad Mahdi, additional, Yang, Zhou, additional, Tu, Yaoquan, additional, Lemoine, Laetitia, additional, Ågren, Hans, additional, Nordberg, Agneta, additional, Långström, Bengt, additional, and Halldin, Christer, additional

Published
2022
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43. First-in-Human Evaluation of 18F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B.

Author

Yuichi Wakabayashi, Stenkrona, Per, Arakawa, Ryosuke, Xuefeng Yan, Van Buskirk, Maia G., Jenkins, Madeline D., Santamaria, Jose A. Montero, Maresca, Kevin P., Akihiro Takano, Liow, Jeih-San, Chappie, Thomas A., Varrone, Andrea, Nag, Sangram, Lei Zhang, Hughes, Zoë A., Schmidt, Christopher J., Doran, Shawn D., Mannes, Andrew, Zanotti-Fregonara, Paolo, and Ooms, Maarten

Published
2022
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46. Target Occupancy Study and Whole-Body Dosimetry with a MAGL PET Ligand 11C-PF-06809247 in non-human Primates

Author

Arakawa, Ryosuke, primary, Takano, Akihiro, additional, Nag, Sangram, additional, Jia, Zhisheng, additional, Amini, Nahid, additional, Maresca, Kevin P, additional, Zhang, Lei, additional, Keliher, Edmund J, additional, Butler, Christopher R, additional, Piro, Justin R, additional, Samad, Tarek A, additional, Smith, Deborah, additional, Nason, Deane, additional, O’Neil, Steve, additional, Trapa, Patrick, additional, Fonseca, Kari R, additional, Litchfield, John, additional, McCarthy, Timothy, additional, Carson, Richard E, additional, and Halldin, Christer, additional

Published
2021
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49. First-in-human evaluation of 18F-PF-06445974, a PET radioligand that preferentially labels phosphodiesterase-4B.

Author

Wakabayashi, Yuichi, Stenkrona, Per, Arakawa, Ryosuke, Xuefeng Yan, Van Buskirk, Maia G., Jenkins, Madeline D., Montero Santamaria, Jose A., Maresca, Kevin P., Takano, Akihiro, Liow, Jeih-San, Chappie, Thomas A., Varrone, Andrea, Nag, Sangram, Lei Zhang, Hughes, Zoë A, Schmidt, Christopher J., Doran, Shawn D., Mannes, Andrew, Zanotti-Fregonara, Paolo, and Ooms, Maarten

Published
2022
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