Neurosteroids and steroid hormones are allosteric modulators of muscarinic receptor

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F21%3A00546861" target="_blank" >RIV/67985823:_____/21:00546861 - isvavai.cz</a>

Alternative codes found

RIV/61388963:_____/21:00546861

Result on the web

<a href="https://doi.org/10.1016/j.neuropharm.2021.108798" target="_blank" >https://doi.org/10.1016/j.neuropharm.2021.108798</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.neuropharm.2021.108798" target="_blank" >10.1016/j.neuropharm.2021.108798</a>

Result language

angličtina

Original language name

Neurosteroids and steroid hormones are allosteric modulators of muscarinic receptor

Original language description

The membrane cholesterol was found to bind and modulate the function of several G-protein coupled receptors including muscarinic acetylcholine receptors. We investigated the binding of 20 steroidal compounds including neurosteroids and steroid hormones to muscarinic receptors. Corticosterone, progesterone and some neurosteroids bound to muscarinic receptors with the affinity of 100 nM or greater. We established a structure-activity relationship for steroid-based allosteric modulators of muscarinic receptors. Further, we show that corticosterone and progesterone allosterically modulate the functional response of muscarinic receptors to acetylcholine at physiologically relevant concentrations. It can play a role in stress control or in pregnancy, conditions where levels of these hormones dramatically oscillate. Allosteric modulation of muscarinic receptors via the cholesterol binding site represents a new pharmacological approach at diseases associated with altered cholinergic signalling.

Czech name

—

Czech description

—

Type

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

CEP classification

—

OECD FORD branch

30105 - Physiology (including cytology)

Project

<a href="/en/project/GA19-05318S" target="_blank" >GA19-05318S: Molecular mechanisms of allosteric modulation of muscarinic acetylcholine receptors by neurosteroids and cholesterol</a><br>

Continuities

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

Publication year

2021

Confidentiality

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

Name of the periodical

Neuropharmacology

ISSN

0028-3908

e-ISSN

1873-7064

Volume of the periodical

199

Issue of the periodical within the volume

Nov 1

Country of publishing house

NL - THE KINGDOM OF THE NETHERLANDS

Number of pages

13

Pages from-to

108798

UT code for WoS article

000703161100007

EID of the result in the Scopus database

2-s2.0-85115393333