All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F17%3A43919283" target="_blank" >RIV/00023752:_____/17:43919283 - isvavai.cz</a>

Result on the web

<a href="https://www.nature.com/articles/s41598-017-05384-z" target="_blank" >https://www.nature.com/articles/s41598-017-05384-z</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1038/s41598-017-05384-z" target="_blank" >10.1038/s41598-017-05384-z</a>

Result language

angličtina

Original language name

All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium

Original language description

Clinical and experimental studies indicate that muscarinic acetylcholine receptors are potential pharmacological targets for the treatment of neurological diseases. Although these receptors have been described in human, bovine and rat cerebral microvascular tissue, a subtype functional characterization in mouse brain endothelium is lacking. Here, we show that all muscarinic acetylcholine receptors (M1-M5) are expressed in mouse brain microvascular endothelial cells. The mRNA expression of M2, M3, and M5 correlates with their respective protein abundance, but a mismatch exists for M1 and M4 mRNA versus protein levels. Acetylcholine activates calcium transients in brain endothelium via muscarinic, but not nicotinic, receptors. Moreover, although M1 and M3 are the most abundant receptors, only a small fraction of M1 is present in the plasma membrane and functions in ACh-induced Ca2+ signaling. Bioinformatic analyses performed on eukaryotic muscarinic receptors demonstrate a high degree of conservation of the orthosteric binding site and a great variability of the allosteric site. In line with previous studies, this result indicates muscarinic acetylcholine receptors as potential pharmacological targets in future translational studies. We argue that research on drug development should especially focus on the allosteric binding sites of the M1 and M3 receptors.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10608 - Biochemistry and molecular biology

Project

<a href="/en/project/LO1611" target="_blank" >LO1611: Sustainability for The National Institute of Mental Health</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2017

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Scientific Reports

ISSN

2045-2322

e-ISSN

—

Volume of the periodical

7

Issue of the periodical within the volume

July

Country of publishing house

GB - UNITED KINGDOM

Number of pages

15

Pages from-to

"Article number: 5083"

UT code for WoS article

000405172600050

EID of the result in the Scopus database

2-s2.0-85023204900