Hippocampal and striatal M1-muscarinic acetylcholine receptors are down-regulated following bilateral vestibular loss in rats

Hippocampus ◽  
2016 ◽  
Vol 26 (12) ◽  
pp. 1509-1514 ◽  
Author(s):  
Phillip Aitken ◽  
Alice Benoit ◽  
Yiwen Zheng ◽  
Bruno Philoxene ◽  
Anne Le Gall ◽  
...  
Keyword(s):  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Vestibular Loss ◽  
Muscarinic Acetylcholine ◽  
Bilateral Vestibular Loss ◽  
M1 Muscarinic

scholarly journals Preparation of a First 18F-Labeled Agonist for M1 Muscarinic Acetylcholine Receptors

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2880 ◽  
Author(s):  
Boris D. Zlatopolskiy ◽  
Felix Neumaier ◽  
Till Rüngeler ◽  
Birte Drewes ◽  
Niklas Kolks ◽  
...  
Keyword(s):  
Acetylcholine Receptors ◽  
Radiochemical Yield ◽  
Muscarinic Acetylcholine Receptors ◽  
Preparative Scale ◽  
Muscarinic Acetylcholine ◽  
Pet Tracer ◽  
Positron Emission ◽  
Diagnostic Applications ◽  
M1 Muscarinic ◽  
Subtype Selective

M1 muscarinic acetylcholine receptors (mAChRs) are abundant in postsynaptic nerve terminals of all forebrain regions and have been implicated in the cognitive decline associated with Alzheimer’s disease and other CNS pathologies. Consequently, major efforts have been spent in the development of subtype-selective positron emission tomography (PET) tracers for mAChRs resulting in the development of several 11C-labeled probes. However, protocols for the preparation of 18F-labeled mAChR-ligands have not been published so far. Here, we describe a straightforward procedure for the preparation of an 18F-labeled M1 mAChR agonist and its corresponding pinacol boronate radiolabeling precursor and the non-radioactive reference compound. The target compounds were prepared from commercially available aryl fluorides and Boc protected 4-aminopiperidine using a convergent reaction protocol. The radiolabeling precursor was prepared by a modification of the Miyaura reaction and labeled via the alcohol-enhanced Cu-mediated radiofluorination. The developed procedure afforded the radiotracer in a non-decay-corrected radiochemical yield of 17 ± 3% (n = 3) and in excellent radiochemical purity (>99%) on a preparative scale. Taken together, we developed a straightforward protocol for the preparation of an 18F-labeled M1 mAChR agonist that is amenable for automation and thus provides an important step towards the routine production of a 18F-labeled M1 selective PET tracer for experimental and diagnostic applications.

scholarly journals Classical and atypical agonists activate M1 muscarinic acetylcholine receptors through common mechanisms

2015 ◽  
Vol 97 ◽  
pp. 27-39 ◽  
Author(s):  
Alena Randáková ◽  
Eva Dolejší ◽  
Vladimír Rudajev ◽  
Pavel Zimčík ◽  
Vladimír Doležal ◽  
...  
Keyword(s):  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Muscarinic Acetylcholine ◽  
M1 Muscarinic

Comparison of subcellular distribution and functions between exogenous and endogenous M1 muscarinic acetylcholine receptors

Life Sciences ◽  
2013 ◽  
Vol 93 (1) ◽  
pp. 17-23 ◽  
Author(s):  
Shigeru Morishima ◽  
Abu Syed Md Anisuzzaman ◽  
Junsuke Uwada ◽  
Hatsumi Yoshiki ◽  
Ikunobu Muramatsu
Keyword(s):  
Subcellular Distribution ◽  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Muscarinic Acetylcholine ◽  
M1 Muscarinic

Novel contribution of cell surface and intracellular M1-muscarinic acetylcholine receptors to synaptic plasticity in hippocampus

2013 ◽  
Vol 126 (3) ◽  
pp. 360-371 ◽  
Author(s):  
Abu Syed Md Anisuzzaman ◽  
Junsuke Uwada ◽  
Takayoshi Masuoka ◽  
Hatsumi Yoshiki ◽  
Matomo Nishio ◽  
...  
Keyword(s):  
Synaptic Plasticity ◽  
Cell Surface ◽  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Muscarinic Acetylcholine ◽  
M1 Muscarinic
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