Nahid Amini

Development of 18F/11C-Labeled Pyrrolo-Pyridine/Pyrimidine LRRK2 Selective PET Radioligands

Sangram Nag, Vladimir Aleksandrovich Stepanov, Akihiro Takano, Ryosuke Arakawa et autres

Background/Objectives: Leucine-rich repeat kinase 2 (LRRK2) is an enzyme implicated in Parkinson’s disease (PD) and a potential therapeutic target. LRRK2 PET radioligands could therefore function as imaging biomarkers for PD and as tools to measure enzyme occupancy of novel therapeutic candidates. This …

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Microsome Mediated in Vitro Metabolism: A Convenient Method for the Preparation of the PET Radioligand Metabolite [18F]FE-PE2I-OH for Translational Dopamine Transporter Imaging

Magnus Schou, Nahid Amini, Akihiro Takano, Ryosuke Arakawa et autres

High Resolution Image Download MS PowerPoint Slide Undesired radiometabolites can be detrimental to the development of positron emission tomography (PET) radioligands. Methods for quantifying radioligand metabolites in brain tissue include ex vivo studies in small animals or labeling and imaging of the …

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

Ryosuke Arakawa, Akihiro Takano, Sangram Nag, Zhisheng Jia et autres

Abstract Background Monoacylglycerol lipase (MAGL) is a key serine hydrolase which terminates endocannabinoid signaling and regulates arachidonic acid driven inflammatory responses within the central nervous system. To develop [ 11 C]PF-06809247 into a clinically usable MAGL positron emission tomography (PET) radioligand, we …

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

Ryosuke Arakawa, Akihiro Takano, Sangram Nag, Zhisheng Jia et autres

Abstract BackgroundMonoacylglycerol lipase (MAGL) is a key serine hydrolase which terminates endocannabinoid signaling and regulates arachidonic acid driven inflammatory responses within the central nervous system (CNS). To develop [11C]PF-06809247 into a clinically usable positron emission tomography (PET) radioligand, we assessed the brain …

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Target Occupancy Study and Whole-Body Dosimetry With a MAGL PET Ligand 11C-PF-06809247 in Non-Human Primates

Ryosuke Arakawa, Akihiro Takano, Sangram Nag, Zhisheng Jia et autres

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Effect of clinically relevant doses of vortioxetine and citalopram on serotonergic PET markers in the nonhuman primate brain

Kai‐Chun Yang, Vladimir Aleksandrovich Stepanov, Nahid Amini, Stefan Martinsson et autres

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Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors

Anton Lindberg, Shuiyu Lu, Sangram Nag, Magnus Schou et autres

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Quantitative Analysis of 18F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain

Akihiro Takano, Laigao M. Chen, Sangram Nag, Michael A. Brodney et autres

β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain and showed high specific binding in …

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Sample preparation techniques for radiometabolite analysis of positron emission tomography radioligands; trends, progress, limitations and future prospects

Mohammad Mahdi Moein, Ryuji Nakao, Nahid Amini, Mohamed Abdel‐Rehim et autres

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The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain

Katarina Varnäs, Anders Juréus, Sjoerd J. Finnema, Peter Johnström et autres

The metabotropic glutamate receptor 5 (mGluR5) is a target for drug development and for imaging studies of the glutamate system in neurological and psychiatric disorders. [11C]AZD9272 is a selective mGluR5 PET radioligand that is structurally different from hitherto applied mGluR5 radioligands. In …

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A Nonhuman Primate PET Study: Measurement of Brain PDE4 Occupancy by Roflumilast Using (R)-[11C]Rolipram

Akihiro Takano, Tolga Uz, Jesus Garcia‐Segovia, Max C. Tsai et autres

Phosphodiesterase 4 (PDE4) inhibition in the brain has been reported to improve cognitive function in animal models. Therefore, PDE4 inhibitors are one of key targets potential for drug development. Investigation of brain PDE4 occupancy would help to understand the effects of PDE4 …

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Development of [Carbonyl-11C]AZ13198083, a Novel Histamine Type-3 Receptor Radioligand with Favorable Kinetics

Kenneth Dahl, Ryuji Nakao, Nahid Amini, Mohammad Mahdi Moein et autres

The histamine subtype-3 receptor (H 3 R) is implicated in a range of central nervous system disorders, and several radioligands have been developed for H 3 R positron emission tomography imaging. However, a limitation of currently used PET radioligands for H 3 …

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