First-in-human assessment of 11c-lsn3172176, an m1 muscarinic acetylcholine receptor pet radiotracer

M Naganawa, N Nabulsi, S Henry… - Journal of Nuclear …, 2021 - Soc Nuclear Med
This was a first-in-human study of the PET radiotracer 11C-LSN3172176 for the muscarinic
acetylcholine receptor subtype M1. The objectives of the study were to determine the …

Evaluation of 11C-LSN3172176 as a novel PET tracer for imaging M1 muscarinic acetylcholine receptors in nonhuman primates

NB Nabulsi, D Holden, MQ Zheng, F Bois… - Journal of Nuclear …, 2019 - Soc Nuclear Med
The M1 muscarinic acetylcholine receptor (mAChR) plays an important role in learning and
memory, and therefore is a target for development of drugs for treatment of cognitive …

[HTML][HTML] [11C]AF150(S), an agonist PET ligand for M1 muscarinic acetylcholine receptors

HJC Buiter, AD Windhorst, MC Huisman, M Yaqub… - EJNMMI research, 2013 - Springer
Background The M1 muscarinic acetylcholine receptor (M1ACh-R) is a G protein-coupled
receptor that can occur in interconvertible coupled and uncoupled states. It is enriched in the …

[HTML][HTML] PET brain kinetics studies of 11C-ITMM and 11C-ITDM, radioprobes for metabotropic glutamate receptor type 1, in a nonhuman primate

T Yamasaki, J Maeda, M Fujinaga, Y Nagai… - American Journal of …, 2014 - ncbi.nlm.nih.gov
The metabotropic glutamate receptor type 1 (mGluR1) is a novel target protein for the
development of new drugs against central nervous system disorders. Recently, we have …

123I-iododexetimide preferentially binds to the muscarinic receptor subtype M1 in vivo

G Bakker, WA Vingerhoets… - Journal of Nuclear …, 2015 - Soc Nuclear Med
The muscarinic M1 receptor (M1R) is highly involved in cognition, and selective M1 agonists
have procognitive properties. Loss of M1R has been found in postmortem brain tissue for …

In vivo quantification of human serotonin 1A receptor using 11C-CUMI-101, an agonist PET radiotracer

MS Milak, C DeLorenzo, F Zanderigo… - Journal of Nuclear …, 2010 - Soc Nuclear Med
The serotonin (5-hydroxytryptamine, or 5-HT) type 1A receptor (5-HT1AR) is implicated in
the pathophysiology of numerous neuropsychiatric disorders. We have published the initial …

[HTML][HTML] Structure–activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine …

A Haider, X Deng, O Mastromihalis, SK Pfister… - … Pharmaceutica Sinica B, 2023 - Elsevier
There is an accumulating body of evidence implicating the muscarinic acetylcholine receptor
4 (M 4) in schizophrenia and dementia with Lewy bodies, however, a clinically validated M 4 …

The PET tracer [11C]MK-6884 quantifies M4 muscarinic receptor in rhesus monkeys and patients with Alzheimer's disease

W Li, Y Wang, TG Lohith, Z Zeng, L Tong… - Science Translational …, 2022 - science.org
Positron emission tomography (PET) ligands play an important role in the development of
therapeutics by serving as target engagement or pharmacodynamic biomarkers. Here, we …

Regional brain uptake of the muscarinic ligand,[18F] FP-TZTP, is greatly decreased in M2 receptor knockout mice but not in M1, M3 and M4 receptor knockout mice

EM Jagoda, DO Kiesewetter, K Shimoji, L Ravasi… - …, 2003 - Elsevier
A muscarinic receptor radioligand, 3-(3-(3-fluoropropyl) thio)-1, 2, 5, thiadiazol-4-yl)-1, 2, 5, 6-
tetrahydro-1-methylpyridine (fP-TZTP) radiolabeled with the positron emitting radionuclide …

Quantification of metabotropic glutamate subtype 5 receptors in the brain by an equilibrium method using 18F-SP203

Y Kimura, FG Siméon, SS Zoghbi, Y Zhang… - Neuroimage, 2012 - Elsevier
A new PET ligand, 3-fluoro-5-(2-(2-18F-(fluoromethyl)-thiazol-4-yl) ethynyl) benzonitrile (18F-
SP203) can quantify metabotropic glutamate subtype 5 receptors (mGluR5) in human brain …