Muscarinic Receptor: From Structure to Animal Models

Mysliveček, J; Jakubík, Ján

doi:10.1007/978-1-4939-2858-3

Cited by 2 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Sixteen‐micrometer‐thick sagittal or frontal sections were cut on a cryostat at −20°C and thaw‐mounted on Superfrost ® Plus glass slides (Carl Roth GmbH & Co. KG, Karlsruhe, Germany) and stored in storage boxes at −80°C until use. For binding to MR, the sections were allowed to thaw and dry for 30 min at 22°C and the density of receptors was determined as previously described (Farar & Myslivecek, 2016; Farar et al., 2012; Valuskova, Farar, Forczek, Krizova, & Myslivecek, 2018). In brief, sections were incubated for 2 h with 2 nM [ 3 H]‐QNB at room temperature.…”

Section: Methodsmentioning

confidence: 99%

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase

et al. 2018

View full text Add to dashboard Cite

ObjectivesM4 muscarinic receptors (MR) presumably play a role in motor coordination. Previous studies have shown different results depending on genetic background and number of backcrosses. However, no attention has been given to biorhythms.Material and MethodsWe therefore analyzed biorhythms under a light/dark cycle obtained telemetrically in intact animals (activity, body temperature) in M4 KO mice growth on the C57Bl6 background using ChronosFit software. Studying pure effects of gene knockout in daily rhythms is especially important knowledge for pharmacological/behavioral studies in which drugs are usually tested in the morning.ResultsWe show that M4 KO mice motor activity does not differ substantially from wild‐type mice during light period while in the dark phase (mice active part of the day), the M4 KO mice reveal biorhythm changes in many parameters. Moreover, these differences are sex‐dependent and are evident in females only. Mesor, night–day difference, and night value were doubled or tripled when comparing female KO versus male KO. Our in vitro autoradiography demonstrates that M4 MR proportion represents 24% in the motor cortex (MOCx), 30% in the somatosensory cortex, 50% in the striatum, 69% in the thalamus, and 48% in the intergeniculate leaflet (IGL). The M4 MR densities were negligible in the subparaventricular zone, the posterior hypothalamic area, and in the suprachiasmatic nuclei.ConclusionsWe conclude that cholinergic signaling at M4 MR in brain structures such as striatum, MOCx, and probably with the important participation of IGL significantly control motor activity biorhythm. Animal activity differs in the light and dark phases, which should be taken into consideration when interpreting the results.

show abstract

Section: Methodsmentioning

confidence: 99%

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase

et al. 2018

View full text Add to dashboard Cite

show abstract

Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole

et al. 2021

View full text Add to dashboard Cite

In this pilot study, a series of new 3,4-dihydroquinolin-2(1H)-one derivatives as potential dopamine receptor D2 (D2R) modulators were synthesized and evaluated in vitro. The preliminary structure–activity relationship disclosed that compound 5e exhibited the highest D2R affinity among the newly synthesized compounds. In addition, 5e showed a very low cytotoxic profile and a high probability to cross the blood–brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of 5e compared to USC-D301, which might be the culprit of the reduced affinity of 5e toward D2R in comparison with USC-D301.

show abstract

Muscarinic Receptor: From Structure to Animal Models

Cited by 2 publications

References 0 publications

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase

Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole

Contact Info

Product

Resources

About

Muscarinic Receptor: From Structure to Animal Models

Cited by 2 publications

References 0 publications

The deletion of M4 muscarinic receptors increases motor activity in females in the dark phase

The deletion of M4 muscarinic receptors increases motor activity in females in the dark phase

Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole

Contact Info

Product

Resources

About

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase

The deletion of M₄ muscarinic receptors increases motor activity in females in the dark phase