GABA-A alpha 2/3 but not alpha 1 receptor subunit ligand inhibits harmaline and pimozide-induced tremor in rats

2023
journal article
article
3
cris.lastimport.wos2024-04-09T20:48:58Z
dc.abstract.enTreatment of tremors, such as in essential tremor (ET) and Parkinson’s disease (PD) is mostly ineffective. Exact tremor pathomechanisms are unknown and relevant animal models are missing. GABA-A receptor is a target for tremorolytic medications, but current non-selective drugs produce side effects and have safety liabilities. The aim of this study was a search for GABA-A subunit-specific tremorolytics using different tremor-generating mechanisms. Two selective positive allosteric modulators (PAMs) were tested. Zolpidem, targeting GABA-A α1, was not effective in models of harmaline-induced ET, pimozide- or tetrabenazine-induced tremulous jaw movements (TJMs), while the novel GABA-A α2/3 selective MP-III-024 significantly reduced both the harmaline-induced ET tremor and pimozide-induced TJMs. While zolpidem decreased the locomotor activity of the rats, MP-III-024 produced small increases. These results provide important new clues into tremor suppression mechanisms initiated by the enhancement of GABA-driven inhibition in pathways controlled by α2/3 but not α1 containing GABA-A receptors. Tremor suppression by MP-III-024 provides a compelling reason to consider selective PAMs targeting α2/3-containing GABA-A receptors as novel therapeutic drug targets for ET and PD-associated tremor. The possibility of the improved tolerability and safety of this mechanism over non-selective GABA potentiation provides an additional rationale to further pursue the selective α2/3 hypothesis.
dc.affiliationWydział Farmaceutyczny : Zakład Chemii Lekówpl
dc.affiliationWydział Nauk o Zdrowiu : Instytut Pielęgniarstwa i Położnictwapl
dc.cm.date2023-03-15T23:20:16Z
dc.cm.id111379pl
dc.cm.idOmegaUJCMca93d7841d0946e8beab8a48b80ba1a7pl
dc.contributor.authorKosmowska, Barbarapl
dc.contributor.authorPaleczna, Martynapl
dc.contributor.authorBiała, Dominika - 191841 pl
dc.contributor.authorKadłuczka, Justynapl
dc.contributor.authorWardas, Jadwigapl
dc.contributor.authorWitkin, Jeffrey M.pl
dc.contributor.authorCook, James M.pl
dc.contributor.authorSharmin, Disharypl
dc.contributor.authorMarcinkowska, Monika - 214403 pl
dc.contributor.authorKuter, Katarzyna Z.pl
dc.date.accession2023-03-15pl
dc.date.accessioned2023-03-15T23:20:16Z
dc.date.available2023-03-15T23:20:16Z
dc.date.issued2023pl
dc.date.openaccess0
dc.description.accesstimew momencie opublikowania
dc.description.number2pl
dc.description.versionostateczna wersja wydawcy
dc.description.volume13pl
dc.identifier.articleid197pl
dc.identifier.doi10.3390/biom13020197pl
dc.identifier.eissn2218-273Xpl
dc.identifier.issn2218-273Xpl
dc.identifier.urihttps://ruj.uj.edu.pl/xmlui/handle/item/309164
dc.identifier.weblinkhttps://www.mdpi.com/2218-273X/13/2/197pl
dc.languageengpl
dc.language.containerengpl
dc.pbn.affiliationDziedzina nauk medycznych i nauk o zdrowiu : nauki farmaceutyczne
dc.rightsUdzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa
dc.rights.licenceCC-BY
dc.rights.simpleviewWolny dostęp
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/legalcode.pl
dc.share.typeOtwarte czasopismo
dc.subject.enresting tremor
dc.subject.enaction tremor
dc.subject.enGABAA alpha 1
dc.subject.enGABAA alpha 2/3
dc.subject.enParkinson’s disease
dc.subject.enessential tremor
dc.subject.enMP-III-024
dc.subject.enzolpidem
dc.subject.enpositive allosteric modulator
dc.subject.entetrabenazine
dc.subtypeArticlepl
dc.titleGABA-A alpha 2/3 but not alpha 1 receptor subunit ligand inhibits harmaline and pimozide-induced tremor in ratspl
dc.title.journalBiomoleculespl
dc.typeJournalArticlepl
dspace.entity.typePublication
cris.lastimport.wos
2024-04-09T20:48:58Z
dc.abstract.en
Treatment of tremors, such as in essential tremor (ET) and Parkinson’s disease (PD) is mostly ineffective. Exact tremor pathomechanisms are unknown and relevant animal models are missing. GABA-A receptor is a target for tremorolytic medications, but current non-selective drugs produce side effects and have safety liabilities. The aim of this study was a search for GABA-A subunit-specific tremorolytics using different tremor-generating mechanisms. Two selective positive allosteric modulators (PAMs) were tested. Zolpidem, targeting GABA-A α1, was not effective in models of harmaline-induced ET, pimozide- or tetrabenazine-induced tremulous jaw movements (TJMs), while the novel GABA-A α2/3 selective MP-III-024 significantly reduced both the harmaline-induced ET tremor and pimozide-induced TJMs. While zolpidem decreased the locomotor activity of the rats, MP-III-024 produced small increases. These results provide important new clues into tremor suppression mechanisms initiated by the enhancement of GABA-driven inhibition in pathways controlled by α2/3 but not α1 containing GABA-A receptors. Tremor suppression by MP-III-024 provides a compelling reason to consider selective PAMs targeting α2/3-containing GABA-A receptors as novel therapeutic drug targets for ET and PD-associated tremor. The possibility of the improved tolerability and safety of this mechanism over non-selective GABA potentiation provides an additional rationale to further pursue the selective α2/3 hypothesis.
dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Leków
dc.affiliationpl
Wydział Nauk o Zdrowiu : Instytut Pielęgniarstwa i Położnictwa
dc.cm.date
2023-03-15T23:20:16Z
dc.cm.idpl
111379
dc.cm.idOmegapl
UJCMca93d7841d0946e8beab8a48b80ba1a7
dc.contributor.authorpl
Kosmowska, Barbara
dc.contributor.authorpl
Paleczna, Martyna
dc.contributor.authorpl
Biała, Dominika - 191841
dc.contributor.authorpl
Kadłuczka, Justyna
dc.contributor.authorpl
Wardas, Jadwiga
dc.contributor.authorpl
Witkin, Jeffrey M.
dc.contributor.authorpl
Cook, James M.
dc.contributor.authorpl
Sharmin, Dishary
dc.contributor.authorpl
Marcinkowska, Monika - 214403
dc.contributor.authorpl
Kuter, Katarzyna Z.
dc.date.accessionpl
2023-03-15
dc.date.accessioned
2023-03-15T23:20:16Z
dc.date.available
2023-03-15T23:20:16Z
dc.date.issuedpl
2023
dc.date.openaccess
0
dc.description.accesstime
w momencie opublikowania
dc.description.numberpl
2
dc.description.version
ostateczna wersja wydawcy
dc.description.volumepl
13
dc.identifier.articleidpl
197
dc.identifier.doipl
10.3390/biom13020197
dc.identifier.eissnpl
2218-273X
dc.identifier.issnpl
2218-273X
dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/309164
dc.identifier.weblinkpl
https://www.mdpi.com/2218-273X/13/2/197
dc.languagepl
eng
dc.language.containerpl
eng
dc.pbn.affiliation
Dziedzina nauk medycznych i nauk o zdrowiu : nauki farmaceutyczne
dc.rights
Udzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa
dc.rights.licence
CC-BY
dc.rights.simpleview
Wolny dostęp
dc.rights.uri
http://creativecommons.org/licenses/by/4.0/legalcode.pl
dc.share.type
Otwarte czasopismo
dc.subject.en
resting tremor
dc.subject.en
action tremor
dc.subject.en
GABAA alpha 1
dc.subject.en
GABAA alpha 2/3
dc.subject.en
Parkinson’s disease
dc.subject.en
essential tremor
dc.subject.en
MP-III-024
dc.subject.en
zolpidem
dc.subject.en
positive allosteric modulator
dc.subject.en
tetrabenazine
dc.subtypepl
Article
dc.titlepl
GABA-A alpha 2/3 but not alpha 1 receptor subunit ligand inhibits harmaline and pimozide-induced tremor in rats
dc.title.journalpl
Biomolecules
dc.typepl
JournalArticle
dspace.entity.type
Publication
Affiliations

* The migration of download and view statistics prior to the date of April 8, 2024 is in progress.

Views
5
Views per month
Views per city
Krakow
3
Downloads
biala_marcinkowska_et-al_gaba-a_alpha_2_3_but_not_alpha_2023.pdf
9