Endogenous ligands of benzodiazepine binding site have inverse agonistic properties

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11130%2F13%3A10196639" target="_blank" >RIV/00216208:11130/13:10196639 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00023001:_____/13:00058765 RIV/00216208:11120/13:43907654

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.mehy.2013.10.006" target="_blank" >http://dx.doi.org/10.1016/j.mehy.2013.10.006</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.mehy.2013.10.006" target="_blank" >10.1016/j.mehy.2013.10.006</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Endogenous ligands of benzodiazepine binding site have inverse agonistic properties

Popis výsledku v původním jazyce

Benzodiazepines have been widely used in clinical praxis for many decades. They act as GABA(A) receptor agonists and possess muscle-relaxant, hypnotic-sedative, anticonvulsant, and anxiolytic properties. Flumazenil acts as a benzodiazepine receptor antagonist (subunits alpha(1), alpha(2), alpha(3), and alpha(5)) or partial agonist (subunits alpha(4) and alpha(6)). It competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversingthe effects of benzodiazepines. In our experiments, administration of flumazenil in rabbits was surprisingly associated with anxiolytic effects similar to those of midazolam. Additionally, flumazenil significantly and dose-dependently decreased the totalnumber of vocalizations in rats, i.e. it was anxiolytic. These observations seem to be in contrast to the effect of flumazenil in humans, where it is believed to produce mainly anxiogenic effects. It seems that in individuals, who exhibi

Název v anglickém jazyce

Endogenous ligands of benzodiazepine binding site have inverse agonistic properties

Popis výsledku anglicky

Benzodiazepines have been widely used in clinical praxis for many decades. They act as GABA(A) receptor agonists and possess muscle-relaxant, hypnotic-sedative, anticonvulsant, and anxiolytic properties. Flumazenil acts as a benzodiazepine receptor antagonist (subunits alpha(1), alpha(2), alpha(3), and alpha(5)) or partial agonist (subunits alpha(4) and alpha(6)). It competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversingthe effects of benzodiazepines. In our experiments, administration of flumazenil in rabbits was surprisingly associated with anxiolytic effects similar to those of midazolam. Additionally, flumazenil significantly and dose-dependently decreased the totalnumber of vocalizations in rats, i.e. it was anxiolytic. These observations seem to be in contrast to the effect of flumazenil in humans, where it is believed to produce mainly anxiogenic effects. It seems that in individuals, who exhibi

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2013

Kód důvěrnosti údajů

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

Název periodika

Medical Hypotheses

ISSN

0306-9877

e-ISSN

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Svazek periodika

81

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

3

Strana od-do

1075-1077

Kód UT WoS článku

000329334800025

EID výsledku v databázi Scopus

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