In vitro binding affinity vs. in vivo site occupancy: A PET study of four diastereomers of dihydrotetrabenazine (DTBZ) in monkey brain-Reference-Cited by-同舟云学术

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In vitro binding affinity vs. in vivo site occupancy: A PET study of four diastereomers of dihydrotetrabenazine (DTBZ) in monkey brain

Published:2021-01 Issue: Volume:92 Page:38-42
ISSN:0969-8051
Container-title:Nuclear Medicine and Biology
language:en
Short-container-title:Nuclear Medicine and Biology

Author:

Kilbourn Michael R.,Cole Erin L.,Scott Peter J.H.

Funder

National Institutes of Health

Adeptio Pharmaceuticals Ltd.

Publisher

Elsevier BV

Subject

Cancer Research,Radiology, Nuclear Medicine and imaging,Molecular Medicine

Reference35 articles.

1. Unbound brain concentrations determine receptor occupancy: a correlation of drug concentration and brain serotonin and dopamine reuptake transporter occupancy for eighteen compounds in rats;Liu;Drug Metab Disp,2009

2. Associating in vitro target binding and in vivo drug occupancy of serotonin reuptake inhibitors: the role of free drug concentrations;Bundgaard;Xenobiotica,2012

3. High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery;Wan;J Med Chem,2007

4. A high-throughput cell-based method to predict the unbound drug fraction in the brain;Mateus;J Med Chem,2014

5. Dopamine transporter (DAT) inhibitors alleviate specific parkinsonian deficits in monkeys: association with DAT occupancy in vivo;Madras;J Pharm Exp Ther,2006

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1. Evaluation of trans- and cis-4-[¹⁸F]Fluorogabapentin for Brain PET Imaging;ACS Chemical Neuroscience;2023-11-10

2. Evaluation oftrans- andcis-4-[¹⁸F]fluorogabapentin for brain PET imaging;2023-09-05

3. 9-Cyclopropylmethoxy-dihydrotetrabenazine and its stereoisomers as vesicular monoamine transporter-2 inhibitors;Future Medicinal Chemistry;2022-07

4. PET Imaging of VMAT2 with the Novel Radioligand [18F]FE-DTBZ-d4 in Nonhuman Primates: Comparison with [11C]DTBZ and [18F]FE-DTBZ;ACS Chemical Neuroscience;2021-11-23

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