Object

Title: Allosteric modulation of serotonin 5-HT1A and 5 HT7 receptors by zinc ions

Abstract:

The first part of the research is devoted to mechanistic insight into the nature of direct Zn interactions with 5 HT1A receptors, investigated with in vitro radioligand experiments and functional assays. The influence of Zn ions on agonist binding was measured by saturation, competition and both association and dissociation kinetic studies using [3H]8-OH-DPAT, also in the functional tests. The obtained results showed zinc non-competitive interactions toward agonist binding site of serotonin 5 HT1A receptors. The biphasic effects, involving potentiation of both agonist binding and function at sub-micromolar concentrations of zinc ions along with the inhibition of agonist affinity at sub-millimolar zinc concentrations, were observed.

Abstract cont.:

In the second part of the thesis, I focus on 5-HT7 receptors. As a result of the research, zinc allosteric inhibition of both agonist and antagonist binding was observed in radioligand binding studies, as well as zinc neutral antagonism at the concentration of 10 μM in the functional assay. Given that zinc potentiation of agonist activity at 5-HT1A receptors and its inhibiting properties on 5-HT7 receptors signaling were detected at low concentrations of zinc ions, it could be hypothesized that these effects may represent the most likely direction of zinc activity under physiological conditions.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmakologia

Degree grantor:

Instytut Farmakologii Polskiej Akademii Nauk.

Promoter:

Andrzej J. Bojarski

Date issued:

2017

Format:

application/pdf

Identifier:

oai:dl.cm-uj.krakow.pl:4235

Call number:

ZB-127777

ControlNumberVIRTUA:

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Language:

pol ; eng

Access rights:

nieograniczony

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego- Collegium Medicum

Object collections:

Last modified:

May 24, 2021

In our library since:

Mar 29, 2018

Number of object content hits:

263

Number of object content views in PDF format

264

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/4236

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ZB-127777 May 24, 2021
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