Article
Pharmacology & Pharmacy
Francesco Petragnano, Irene Fasciani, Clotilde Mannoury la Cour, Benjamin di Cara, Gabriella Aloisi, Marco Carli, Shivakumar Kolachalam, Mario Rossi, Francesco Marampon, Marco Scarselli, Mark J. Millan, Roberto Maggio
Summary: This study investigates the affinity and activation of (+)-4-Propyl-9-hydroxynaphthoxazine on various monoamine receptors. It is found to have high affinity for hD(4.4), h5-HT1A, and h5-HT7 receptors, as well as hD(3) and hD(2L) receptors. It also strongly activates dopamine hD(3)-hD(2L) heterodimers. These findings are important for interpreting PET studies and may have implications for the treatment of Parkinson's disease and other disorders.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Neurosciences
Yasuharu Yamamoto, Keisuke Takahata, Manabu Kubota, Harumasa Takano, Hiroyoshi Takeuchi, Yasuyuki Kimura, Yasunori Sano, Shin Kurose, Hiroshi Ito, Masaru Mimura, Makoto Higuchi
Summary: The study revealed a significant positive correlation between DA synthesis capacity and DA transporter availability in the putamen, but no significant correlation between DA synthesis capacity and D2 receptor availability in the striatum, indicating a relationship between DA synthesis capacity and reuptake, while the total abundance of D2 receptors may not directly participate in the regulatory mechanism.
Article
Biochemistry & Molecular Biology
Chi-Hyeon Yoo, Zhen Chen, Nisha Rani, Jiahui Chen, Jian Rong, Laigao Chen, Lei Zhang, Steven H. Liang, Hsiao-Ying Wey
Summary: This study evaluated the methods of PET quantification for [18F]PF-06455943, a radioligand for LRRK2 imaging. The results showed that a two-tissue compartmental model and a Logan graphical analysis were appropriate for PET quantification. Additionally, it was found that total distribution volume (VT) values could be reliably estimated with as short as a 30 min scan duration. Homologous blocking studies confirmed the specific binding of [18F]PF-06455943 and revealed that the nonradioactive mass of PF-06455943 achieved 45-55% of VT displacement in the whole brain. This work supports the translation of [18F]PF-06455943 PET imaging for the human brain and target occupancy studies.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Engineering, Mechanical
Chi-Hyeon Yoo, Zhen Chen, Nisha Rani, Jiahui Chen, Jian Rong, Laigao Chen, Lei Zhang, Steven H. Liang, Hsiao-Ying Wey
Summary: Mutations in the LRRK2 gene are common causes of inherited Parkinson's disease. A novel PET radioligand, [F-18]PF-06455943, has been developed for LRRK2 imaging. The quantification methods for [F-18]PF-06455943 PET imaging in nonhuman primate brains have been evaluated, and the specific binding of the radioligand has been confirmed.
JOURNAL OF FLUIDS AND STRUCTURES
(2023)
Article
Neurosciences
Katina C. Calakos, Aleksandra Rusowicz, Brian Pittman, Jean-Dominique Gallezot, Marc N. Potenza, Kelly P. Cosgrove, David Matuskey
Summary: Social factors are associated with psychiatric outcomes and brain function. This study found that living in a populous area with fewer educational resources may lead to higher availability of dopamine D2/3 receptors. This suggests that the social environment has an impact on an individual's brain function.
NEUROSCIENCE LETTERS
(2022)
Article
Neurosciences
Kyoji Okita, Koichi Kato, Yoko Shigemoto, Noriko Sato, Toshihiko Matsumoto, Hiroshi Matsuda
Summary: This study aims to investigate the impact of the A2A receptor antagonist istradefylline on dopamine D2-type receptor availability and impulsivity in the human brain, hypothesizing that it will increase D2-type BPND and improve impulsivity control. The double-blind, randomized controlled trial will involve 40 healthy participants receiving either istradefylline or placebo for two weeks, with PET scans and neuropsychological measurements conducted to evaluate the outcomes. The findings will be disseminated through peer reviewed scientific journals and conferences.
FRONTIERS IN NEUROSCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Ahmed Haider, Lu Wang, Luca Gobbi, Yinlong Li, Ahmad Chaudhary, Xin Zhou, Jiahui Chen, Chunyu Zhao, Jian Rong, Zhiwei Xiao, Lu Hou, Nehal H. Elghazawy, Wolfgang Sippl, April T. Davenport, James B. Daunais, Hazem Ahmed, Ron Crowe, Michael Honer, Axel Rominger, Uwe Grether, Steven H. Liang, Simon M. Ametamey
Summary: The study focuses on the performance characteristics of [F-18]RoSMA-18-d(6) in nonhuman primates (NHPs) and its potential as a PET radioligand for imaging CB2. The results show high binding of [F-18]RoSMA-18-d(6) to CB2 in NHP spleen tissue, indicating its suitability for CB2 mapping. The study also suggests the potential utility of [F-18]RoSMA-18-d(6) in probing CB2-expressing cells in the bone marrow.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Substance Abuse
Simon Jangard, Nitya Jayaram-Lindstrom, Nils Hentati Isacsson, Granville James Matheson, Pontus Plaven-Sigray, Johan Franck, Jacqueline Borg, Lars Farde, Simon Cervenka
Summary: This study found no significant association between striatal dopamine D2 receptor availability and later alcohol use or alcohol-related factors. However, there was a negative association between D2 receptor availability and later impulsivity, although the effect size was small.
Article
Neurosciences
Kyoungjune Pak, Lauri Nummenmaa
Summary: This study investigated the association between dopamine receptor availability and overweight/obesity using Bayesian and frequentist meta-analysis. The results showed that there was no difference in dopamine receptor availability between lean and overweight/obese subjects, but this effect was dependent on the radiopharmaceutical and the degree of obesity.
HUMAN BRAIN MAPPING
(2023)
Article
Medicine, Research & Experimental
Aisling M. Chaney, Francisco R. Lopez-Picon, Sophie Serriere, Rui Wang, Daniela Bochicchio, Samuel D. Webb, Matthias Vandesquille, Michael K. Harte, Christina Georgiadou, Catherine Lawrence, Julie Busson, Johnny Vercouillie, Clovis Tauber, Frederic Buron, Sylvain Routier, Tristan Reekie, Anniina Snellman, Michael Kassiou, Johanna Rokka, Karen E. Davies, Juha O. Rinne, Dervis A. Salih, Frances A. Edwards, Llwyd D. Orton, Stephen R. Williams, Sylvie Chalon, Herve Boutin
Summary: The TgF344-AD rat model shows improved AD pathology modeling, including neuronal loss and Tau accumulation, with alterations in neuroinflammation and cholinergic receptors observed in vivo. This model can be useful for assessing early neurotransmission dysfunction and neuroinflammation in AD longitudinally, showing a potential for PET detection of Tau pathology.
Article
Clinical Neurology
Hironori Nishibe, Amane Tateno, Takeshi Sakayori, Masahiro Yamamoto, WooChan Kim, Hiroyoshi Kakuyama, Yoshiro Okubo
Summary: Transdermal antipsychotic patch formulations, specifically blonanserin patches at doses of 40 mg/d and 80 mg/d, exhibit lower diurnal variability in occupancy compared to blonanserin tablets at doses of 8 mg/d and 16 mg/d, indicating that patches may be a suitable alternative for patients with schizophrenia. The study suggests that blonanserin patches could potentially offer a new treatment option for these patients.
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
(2021)
Article
Multidisciplinary Sciences
Naohisa Miyakawa, Yuji Nagai, Yukiko Hori, Koki Mimura, Asumi Orihara, Kei Oyama, Takeshi Matsuo, Ken-ichi Inoue, Takafumi Suzuki, Toshiyuki Hirabayashi, Tetsuya Suhara, Masahiko Takada, Makoto Higuchi, Keisuke Kawasaki, Takafumi Minamimoto
Summary: Pharmacological and surgical treatments of epilepsy have limited success, therefore a more targeted and on-demand approach is desired. The authors demonstrate the use of inhibitory chemogenetics to attenuate cortical seizures and subsequent convulsions in nonhuman primates. These results highlight the efficacy of DREADDs for treating epilepsy in a primate model.
NATURE COMMUNICATIONS
(2023)
Article
Pharmacology & Pharmacy
Kyoji Okita, Toshihiko Matsumoto, Daisuke Funada, Maki Murakami, Koichi Kato, Yoko Shigemoto, Noriko Sato, Hiroshi Matsuda
Summary: This study aims to assess the effect of the selective A2A receptor antagonist, istradefylline, on D2-type BPND in the striatum and neuroinflammation in the whole brain of individuals with methamphetamine use disorder. The hypotheses are that istradefylline will increase striatal D2-type BPND and attenuate neuroinflammation.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Michael R. Kilbourn
Summary: The application of positron emission tomography (PET) imaging to study brain biochemistry, especially dopamine neurotransmission, has significantly grown over the past 40 years. PET imaging of dopaminergic functions in the central nervous system is routinely used for research in neurology, psychiatry, drug abuse and addiction, as well as drug development. The key advancement in PET imaging is the development of unique radiotracers labeled with positron-emitting radionuclides like carbon-11 and fluorine-18, which have greatly contributed to the progress in this field.
Article
Behavioral Sciences
Yasmin Zakiniaeiz, Ralitza Gueorguieva, MacKenzie R. Peltier, Terril L. Verplaetse, Walter Roberts, Sherry A. McKee, Kelly P. Cosgrove
Summary: Sex differences exist in tobacco smoking, with women having greater difficulty quitting smoking than men. This study found that lower estradiol levels in women were associated with lower dopamine levels in the dlPFC, which may contribute to the difficulty in resisting smoking.
FRONTIERS IN BEHAVIORAL NEUROSCIENCE
(2023)