Article
Chemistry, Multidisciplinary
Esmaeil Gharepapagh, Ashraf Fakhari, Tahereh Firuzyar, Ashkan Shomali, Farzaneh Azimi
Summary: A new Tc-99m N-doped graphene quantum dot Tc-99m-(N-GQD) moiety has been developed for possible radiolabeling of molecules with chelation limitations and poor water solubility. The Tc-99m-(N-GQDs) were synthesized and characterized with high purity, demonstrating high radiochemical purity after radiolabeling and effective elimination by kidneys in biodistribution studies. Dosimetry studies showed kidneys as critical organs for the effective radiation dose of Tc-99m-(N-GQDs).
NEW JOURNAL OF CHEMISTRY
(2021)
Review
Immunology
Mohammed Alrouji, Hayder M. Al-Kuraishy, Ali I. Al-Gareeb, Hebatallah M. Saad, Gaber El-Saber Batiha
Summary: Parkinson's disease (PD) is a degenerative disorder caused by the damage to certain neurons in the brain. The use of non-steroidal anti-inflammatory drugs (NSAIDs) to treat musculoskeletal problems in PD patients can have both beneficial and harmful effects on the progression of the disease. NSAIDs can potentially prevent the development of PD by reducing neuroinflammation, but they may also inhibit neuroprotective mechanisms and worsen neuroinflammation. In conclusion, the effect of NSAIDs on PD neuropathology is still uncertain and further research is needed.
INFLAMMOPHARMACOLOGY
(2023)
Review
Clinical Neurology
Fabiola Atzeni, Ignazio F. Masala, Michela Bagnasco, Luigi Lanata, Flavio Mantelli, Piercarlo Sarzi-Puttini
Summary: A new meta-analysis comparing ketoprofen and ibuprofen in patients with RA found that ketoprofen was more effective in managing RA pain at therapeutic doses. There were no significant differences between the two drugs in terms of tolerability or safety based on the studies included in the meta-analysis.
Review
Biochemistry & Molecular Biology
Domenica Francesca Mariniello, Valentino Allocca, Vito D'Agnano, Riccardo Villaro, Luigi Lanata, Michela Bagnasco, Luigi Aronne, Andrea Bianco, Fabio Perrotta
Summary: COVID-19 is an infectious disease caused by SARS-CoV-2, and early treatment is crucial in influencing the clinical course of the disease. Non-steroidal anti-inflammatory drugs are the mainstay of early phase treatment for COVID-19.
Article
Chemistry, Applied
Lili Song, Zhigang Liu, Minjie Liu, Pei Tang, Fener Chen
Summary: The practical synthesis of ketoprofen, a representative nonsteroidal anti-inflammatory drug, has been achieved with an overall yield of 44% on a decagram scale. This synthetic approach involves the use of TiCl4-Et3N mediated aldol/enollactonization annulation for dihydrobenzofuranone core formation, and a highly efficient pyrolytic aromatization condition for the construction of the vital 2-arylpropionic acid (2-APA) moiety. The avoidance of hazardous chemicals and crystallization of several intermediates is beneficial for the scalable synthesis of ketoprofen.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2023)
Article
Medicine, Research & Experimental
Katarzyna Potyrak, Benita Wiatrak, Edward Krzyzak, L. Lukasz Szczukowski, Piotr Swiatek, Adam Szelag
Summary: Alzheimer's disease remains a serious disorder with no effective therapy. However, certain compounds show potential for beneficial effects on damaged neuronal cells and are capable of crossing the blood-brain barrier.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Biophysics
Leticia Massimo Pereira, Natalia Cristina Gomes-da-Silva, Martha Sahyli Ortega Pijeira, Filipe Leal Portilho, Andrezza Santos Cordeiro, Luciana Magalhaes Rebelo Alencar, Luana Barbosa Correa, Maria das Gracas Henriques, Ralph Santos-Oliveira, Elaine Cruz Rosas
Summary: Arthritis is a chronic disease that affects approximately 1% of the global population. The main therapies available for this condition have a high risk of failure and advanced treatments are limited and expensive. In this study, nanomicelles of a plant-derived compound called Methyl gallate (MG) were formulated and evaluated for their effectiveness in a mice model of arthritis. The nanomicelles showed promising results in reducing inflammation and cell count at the inflammation site. These findings suggest that MG nanomicelles could be a potential alternative treatment for arthritis.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Martin Bauer, Sandra Barna, Matthias Blaickner, Konstantin Prosenz, Karsten Bamminger, Verena Pichler, Nicolas Tournier, Marcus Hacker, Markus Zeitlinger, Georgios Karanikas, Oliver Langer
Summary: The new PET tracer [C-11]metoclopramide showed predominant uptake in the liver with renal and biliary excretion of radioactivity. The mean effective dose was comparable to other C-11-labeled PET tracers, and the urinary bladder and liver received the highest radiation doses. Overall, [C-11]metoclopramide was found to be safe and well tolerated in healthy adults.
MOLECULAR IMAGING AND BIOLOGY
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tuula Tolvanen, Kari Kalliokoski, Simona Malaspina, Anna Kuisma, Salla Lahdenpohja, Ernst J. Postema, Matthew P. Miller, Mika Scheinin
Summary: The study investigated the safety, biodistribution, and internal radiation dosimetry of a novel F-18-labeled radiohybrid PSA imaging agent in healthy volunteers, showing favorable results for PET imaging.
JOURNAL OF NUCLEAR MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Vandna, Shruti Ahlawat, Krishna Kant Sharma, Hari Mohan
Summary: This study found that the co-administration of ketoprofen with Yersinia enterocolitica can cause significant damage to the rat gut, leading to altered expression of gut proteins and profound effects on the NF-kB signaling pathway, immune system, dysbiosis, and gut injury. Additionally, the biochemical and histopathological analysis of treated rats showed evidence of liver enzyme activity alteration and behavioral response changes, indicating the detrimental effects of the co-administration.
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2022)
Article
Medicine, Research & Experimental
Su Bin Kim, Min Seob Lee, In Ho Song, Hyun Soo Park, Sang Eun Kim
Summary: This study validated iodine uptakes and investigated theranostic surrogacy using DTC xenograft mouse models and SPECT imaging. Dosimetry was determined by simulating energy deposition/dose distribution and estimating absorbed dose. The study is expected to improve the challenging dosimetry process in clinical use.
MOLECULAR PHARMACEUTICS
(2023)
Article
Clinical Neurology
Glen Liau Zi Qiang, Sherry Liu Jiani, Wing Moon Raymond Lam, Jiayi Weng, Lucius Ho Kang Hua, Louise Kok, Syeda Fabeha Husain, Ling Liu, Sanjay Khanna, Hee Kit Wong
Summary: This study investigates the effectiveness of systemic nonsteroidal anti-inflammatory drugs in reducing neuroinflammation induced by recombinant human bone morphogenetic protein-2 in rodent models. The results show that the intervention groups have reduced seroma volume and inflammatory markers, and improved functional measures of neuroinflammation compared to the control group.
Article
Radiology, Nuclear Medicine & Medical Imaging
Aline Delva, Michel Koole, Kim Serdons, Guy Bormans, Longbin Liu, Jonathan Bard, Vinod Khetarpal, Celia Dominguez, Ignacio Munoz-Sanjuan, Andrew Wood, Mette Skinbjerg, Yuchuan Wang, Wim Vandenberghe, Koen Van Laere
Summary: In this study, the biodistribution and dosimetry of two tracers designed for PET imaging of aggregated mutant huntingtin (mHTT) in the brain were investigated in healthy volunteers. The results suggest that both tracers are safe for in vivo PET imaging in humans. One tracer showed promising kinetic properties in the brain, while the other may accumulate a brain-penetrant metabolite.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Review
Biochemistry & Molecular Biology
Mihai Ruscu, Andreea Cercel, Ertugrul Kilic, Bogdan Catalin, Andrei Gresita, Dirk M. Hermann, Carmen Valeria Albu, Aurel Popa-Wagner
Summary: Ischemic stroke treatment can be improved with the use of nanomedicines, which have been shown to reduce infarct size and improve neurological function in animal models. This systematic review evaluates the efficacy of nanoparticle-based treatments for ischemic stroke and their potential impact on future therapies. The review also assesses the scientific quality of current research in this field.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Computer Science, Artificial Intelligence
Jaewon Yang, Jae Ho Sohn, Spencer C. Behr, Grant T. Gullberg, Youngho Seo
Summary: This study demonstrates the feasibility of CT-less attenuation and scatter correction in whole-body PET using deep learning, highlighting the potential benefits and pitfalls. Results show that deep learning-corrected PET images exhibit high similarity with ASC-corrected PET, but also reveal potential issues such as radiation dose reduction and artifact removal, as well as possible false-negative and false-positive results.
RADIOLOGY-ARTIFICIAL INTELLIGENCE
(2021)
Article
Biochemical Research Methods
Miki Goto, Akira Nishiyama, Takao Yamaguchi, Kyosuke Watanabe, Kenji Fujii, Yasuyoshi Watanabe, Hisashi Doi
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
(2019)
Article
Biochemistry & Molecular Biology
Kyosuke Watanabe, Satoshi Nozaki, Mild Goto, Ken-ichi Kaneko, Emi Hayashinaka, Satsuki Irie, Akira Nishiyama, Kazuaki Kasai, Kenji Fujii, Yasuhiro Wada, Kei Mizuno, Kenji Mizuseki, Hisashi Doi, Yasuyoshi Watanabe
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2019)
Article
Biochemical Research Methods
Takayuki Ose, Joonas A. Autio, Masahiro Ohno, Kantaro Nishigori, Nobuyoshi Tanki, Ami Igesaka, Tomoko Mori, Hisashi Doi, Yasuhiro Wada, Iwao Nakajima, Hiroshi Watabe, Takuya Hayashi
JOURNAL OF NEUROSCIENCE METHODS
(2019)
Article
Multidisciplinary Sciences
Satoshi Nozaki, Yuka Nakatani, Aya Mawatari, Nina Shibata, William E. Hume, Emi Hayashinaka, Yasuhiro Wada, Hisashi Doi, Yasuyoshi Watanabe
SCIENTIFIC REPORTS
(2019)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tomohiko Yamane, Kenji Fukushima, Suguru Shirotake, Koshiro Nishimoto, Takashi Okabe, Masafumi Oyama, Akira Seto, Ichiei Kuji
Summary: This study aimed to evaluate the test-retest repeatability of SUV in bone SPECT/CT in clinical settings. The results showed an almost perfect correlation between repeated SUVmax and SUVpeak measurements, indicating their reliability as indicators in patient management.
ANNALS OF NUCLEAR MEDICINE
(2021)
Correction
Biochemistry & Molecular Biology
Yasuyoshi Watanabe, Aya Mawatari, Kazuki Aita, Yuzuru Sato, Yasuhiro Wada, Takayoshi Nakaoka, Kayo Onoe, Emi Yamano, Go Akamatsu, Akihito Ohnishi, Keiji Shimizu, Masahiro Sasaki, Hisashi Doi, Michio Senda
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Yasuyoshi Watanabe, Aya Mawatari, Kazuki Aita, Yuzuru Sato, Yasuhiro Wada, Takayoshi Nakaoka, Kayo Onoe, Emi Yamano, Go Akamatsu, Akihito Ohnishi, Keiji Shimizu, Masahiro Sasaki, Hisashi Doi, Michio Senda
Summary: This study investigated the whole-body pharmacokinetics of [C-11]TTFD in human healthy volunteers using PET imaging and radiation dosimetry. The results showed different uptake patterns of the compound in various tissues, with a relatively low effective radiation dose calculated.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Chemistry, Medicinal
Shuhei Takatani, Tsuyoshi Tahara, Mieko Tsuji, Daiki Ozaki, Nina Shibata, Yoshinobu Hashizume, Masaaki Suzuki, Hirotaka Onoe, Yasuyoshi Watanabe, Hisashi Doi
Summary: Efficient synthesis of L-[5-C-11]leucine and L-alpha-[5-C-11]methylleucine was achieved using a two-step sequence, with promising potential of L-alpha-[5-C-11]methylleucine as a probe for visualizing tumors confirmed through tissue distribution analysis.
Article
Chemistry, Organic
Hisashi Doi, Miki Goto, Yuzuru Sato
Summary: A rapid Pd-0-mediated cross-coupling reaction was reported for synthesizing C-11-acetic acid and its corresponding imidyl esters as radiolabeling reagents. The reaction yielded [C-11]2 with satisfactory radioactivity and good yield, suitable for in vivo imaging studies. The injectable radiopharmaceutical formulation of [C-11]2 prepared using 33 GBq of [C-11]CH3I showed a decay-corrected radiochemical yield of 63-73%, providing potential applications in positron emission tomography studies.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Takayoshi Nakaoka, Ken-ichi Kaneko, Satsuki Irie, Aya Mawatari, Ami Igesaka, Yuta Uetake, Hidenori Ochiai, Takashi Niwa, Emi Yamano, Yasuhiro Wada, Masaaki Tanaka, Kohei Kotani, Hideki Kawahata, Joji Kawabe, Yukio Miki, Hisashi Doi, Takamitsu Hosoya, Maeda Kazuya, Hiroyuki Kusuhara, Yuichi Sugiyama, Yasuyoshi Watanabe
Summary: Uptake and efflux transporters play crucial roles in drug disposition. PET imaging is a useful tool for directly assessing drug transporter activity. A synthetic method for [18F]PTV, a PET probe for hepatobiliary transport, was developed. Rifampicin pretreatment significantly inhibited hepatic concentration and biliary excretion of the probe and decreased hepatic uptake clearance and canalicular efflux clearance. These results demonstrate the usefulness of [18F]PTV for investigating hepatobiliary transporters in humans.
DRUG METABOLISM AND PHARMACOKINETICS
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ken-ichi Kaneko, Satsuki Irie, Aya Mawatari, Ami Igesaka, Di Hu, Takayoshi Nakaoka, Emi Hayashinaka, Yasuhiro Wada, Hisashi Doi, Yasuyoshi Watanabe, Yilong Cui
Summary: This study quantitatively analyzed the spatiotemporal changes in neuroinflammation after status epilepticus in rats, using TSPO PET imaging. The results provide valuable evidence for developing new anti-inflammatory therapies for epilepsy, with activated microglia identified as a crucial therapeutic target in the early phase after status epilepticus.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Multidisciplinary Sciences
Kayo Takahashi, Takamitsu Hosoya, Kayo Onoe, Tomoko Mori, Shusaku Tazawa, Aya Mawatari, Yasuhiro Wada, Yumiko Watanabe, Hisashi Doi, Yasuyoshi Watanabe
Summary: This study synthesized three analogs of cetrozole for PET imaging of aromatase in the brain, with iso-cetrozole showing the most promising results. The inhibitory activities of the analogs correlated well with their binding potentials to aromatase in animal models, and iso-cetrozole demonstrated faster metabolism in brain tissue compared to cetrozole.
SCIENTIFIC REPORTS
(2021)
Article
Biochemistry & Molecular Biology
Satoshi Nozaki, Yuka Nakatani, Aya Mawatari, William E. Hume, Yasuhiro Wada, Akira Ishii, Masaaki Tanaka, Naohiro Tsuyuguchi, Hisashi Doi, Yasuyoshi Watanabe
Summary: In this first-in-human PET study, the biodistribution and tumor accumulation of a novel PET probe, F-18-FIMP, were evaluated. The results showed rapid excretion of F-18-FIMP from the kidneys and no characteristic physiological accumulation in healthy controls. Compared with other probes, F-18-FIMP provided clearer imaging in patients with brain tumors.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tomohiko Yamane, Yohji Matsusaka, Kenji Fukushima, Akira Seto, Ichiro Matsunari, Ichiei Kuji
Summary: This article introduces the application of positron emission tomography (PET) in oncology and emphasizes the importance of recognizing the patterns of solitary or asymmetrical skeletal muscle uptake seen in routine scans.
JAPANESE JOURNAL OF RADIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Tatsuya Kida, Nobuaki Takahashi, Masayuki X. Mori, Jiacheng H. Sun, Hideto Oota, Kosuke Nishino, Takashi Okauchi, Yuta Ochi, Daisuke Kano, Ukihide Tateishi, Yasuyoshi Watanabe, Yilong Cui, Yasuo Mori, Hisashi Doi
Summary: TRPV1-targeted compounds were synthesized by modifying the structure of SB366791, and higher antagonistic activities were achieved by avoiding amide-iminol tautomerization. Additionally, explorative PET imaging trials were conducted using labeled derivatives, providing a basis for further applications.
RSC MEDICINAL CHEMISTRY
(2022)