Facile synthesis of new carbon-11 labeled conformationally restricted rivastigmine analogues as potential PET agents for imaging AChE and BChE enzymes

Wang, Min; Wang, Ji Quan; Gao, Mingzhang; Zheng, Qi‐Huang

doi:10.1016/j.apradiso.2007.11.005

Cited by 8 publications

(4 citation statements)

References 24 publications

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“…In addition, a limited literature search was performed on reported values of SA for carbon-11 methylations. In the search we found six articles from four different groups, all articles described radiopharmaceuticals produced from [ 11 C]CO 2 [95][96][97][98][99][100] . The reported SA ranged from 56 to 222 GBq/µmol at EOB for five of the articles, which is very much in line with the SA from our in-house [ 11 C]CO 2 production reported in Table 2.…”

Section: Specific Radioactivity: [ 11 C]ch 3 I (Paper I)mentioning

confidence: 99%

[11C]AZ10419369: A selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain

et al. 2008

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Section: Specific Radioactivity: [ 11 C]ch 3 I (Paper I)mentioning

confidence: 99%

[11C]AZ10419369: A selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain

et al. 2008

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“…Therefore, the authors pro posed their potential application as tracers for cardiac imaging of AChE and BuChE. Thi highlights the importance of designing drugs/tracers that can effectively cross the BBB when targeting the CNS in neurodegenerative disorders [109]. This type of inhibitor, benzoisoxazole lactam derivative 95, demonstrated potent in vitro enzyme inhibition in the sub-nanomolar range compared to other related AChE inhibitors containing N-benzylpiperidine with indanone (92) [98], benzoisoxazoles (94) [107], or indoles (93) [108] groups (Figure 16).…”

Section: First Class Of Ache's Pet Probes (Labeled Acheis)mentioning

confidence: 99%

“…Therefore, the authors proposed their potential application as tracers for cardiac imaging of AChE and BuChE. This highlights the importance of designing drugs/tracers that can effectively cross the BBB when targeting the CNS in neurodegenerative disorders [109]. Wang et al developed a 11 C-radiosynthesis method for conformationally restricted quaternary ammonium rivastigmine analogues to image both AChE and BuChE (Figure 17, 101), based on a newer generator inhibitor with dual activity on both enzymes.…”

Section: First Class Of Ache's Pet Probes (Labeled Acheis)mentioning

confidence: 99%

“…Therefore, the authors proposed their potential application as tracers for cardiac imaging of AChE and BuChE. This highlights the importance of designing drugs/tracers that can effectively cross the BBB when targeting the CNS in neurodegenerative disorders [109]. In vitro and in vivo experiments were conducted using these compounds in mice to study the distribution and activity of AChE.…”

Section: First Class Of Ache's Pet Probes (Labeled Acheis)mentioning

confidence: 99%

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New Advances in the Exploration of Esterases with PET and Fluorescent Probes

Gil-Rivas,

de Pascual-Teresa,

Ortín

et al. 2023

Molecules

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Esterases are hydrolases that catalyze the hydrolysis of esters into the corresponding acids and alcohols. The development of fluorescent probes for detecting esterases is of great importance due to their wide spectrum of biological and industrial applications. These probes can provide a rapid and sensitive method for detecting the presence and activity of esterases in various samples, including biological fluids, food products, and environmental samples. Fluorescent probes can also be used for monitoring the effects of drugs and environmental toxins on esterase activity, as well as to study the functions and mechanisms of these enzymes in several biological systems. Additionally, fluorescent probes can be designed to selectively target specific types of esterases, such as those found in pathogenic bacteria or cancer cells. In this review, we summarize the recent fluorescent probes described for the visualization of cell viability and some applications for in vivo imaging. On the other hand, positron emission tomography (PET) is a nuclear-based molecular imaging modality of great value for studying the activity of enzymes in vivo. We provide some examples of PET probes for imaging acetylcholinesterases and butyrylcholinesterases in the brain, which are valuable tools for diagnosing dementia and monitoring the effects of anticholinergic drugs on the central nervous system.

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PET probes for imaging brain acetylcholinesterase

Kikuchi¹,

Okamura²,

Zhang³

et al. 2013

Labelled Comp Radiopharmac

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Imaging acetylcholinesterase (AChE) is valuable not only for diagnosing and understanding dementia but also for monitoring the effects of cholinesterase inhibitors used as antidementia drugs and for determining the appropriate clinical dosage of newly developed cholinesterase inhibitors. The distribution of AChE in the living brain can be imaged with two different types of radioprobes, including substrate-type and ligand-type probes. The substrate-type positron emission tomography (PET) probes, N-[(11) C]methylpiperidin-4-yl acetate ([(11) C]MP4A), and its propionate, [(11) C]MP4P, have been widely used in clinical studies of dementia, including Alzheimer's disease. [(11) C]MP4A and [(11) C]MP4P have been used to demonstrate a reduction in AChE activity in the brains of dementia patients, as well as the bioavailability of AChE inhibitors, leading to the subsequent development of the widely available (18) F-labeled derivatives of MP4A. In addition, several radiolabeled cholinesterase inhibitors have been developed as PET probes for AChE mapping in the brain. Herein, we have reviewed the development of PET probes for the imaging of AChE in the brain and described the principles of measuring AChE activity in the brain using PET with substrate-type radioprobes. A discussion of the reagents developed from substrate-type PET probes for the specific measurement of AChE activity in vitro has also been provided.

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Facile synthesis of new carbon-11 labeled conformationally restricted rivastigmine analogues as potential PET agents for imaging AChE and BChE enzymes

Cited by 8 publications

References 24 publications

[11C]AZ10419369: A selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain

[11C]AZ10419369: A selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain

New Advances in the Exploration of Esterases with PET and Fluorescent Probes

PET probes for imaging brain acetylcholinesterase

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