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Voltage-clamp evidence of GABA

Authors :
Hélder, Fernandes
Vânia, Batalha
Ellen, Braksator
Simon, Hebeisen
Maria João, Bonifácio
Maria Augusta, Vieira-Coelho
Patrício, Soares-da-Silva
Source :
Pharmacological reports : PR. 74(5)
Publication Year :
2022

Abstract

Anxiolytic benzodiazepines, due to their clinical effectiveness, are one of the most prescribed drugs worldwide, despite being associated with sedative effects and impaired psychomotor and cognitive performance. Not every GABAThe present study pharmacodynamically evaluated chlornordiazepam, the main active metabolite of mexazolam, upon GABAAs shown by whole-cell patch-clamp data, chlornordiazepam potentiated GABA-evoked current amplitude in α2 and α3 containing receptors without changing the current amplitude in α1 containing receptors. However, current decay time increased, particularly in GABAThis novel evidence demonstrates that mexazolam (through its main metabolite chlornordiazepam) has a "pharmacodynamic fingerprint" that correlates better with an anxiolytic profile and fewer sedative effects, when compared to alprazolam, bromazepam and zolpidem, explaining clinical trial outcomes with these drugs. This also highlights the relevance of the pharmacological selectivity over GABA

Details

ISSN :
22995684
Volume :
74
Issue :
5
Database :
OpenAIRE
Journal :
Pharmacological reports : PR
Accession number :
edsair.pmid..........d7dfd3dc6bf1ad87169d7ca84b541e8c