ArticleActa pharmacologica Sinica2012
Differential effects of short- and long-term zolpidem treatment on recombinant α1β2γ2s subtype of GABA(A) receptors in vitro.
Article in Acta pharmacologica Sinica, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 8 citations in OpenAlex.
- Molecular Mechanisms and Probe-Dependent Effects of Clinically Relevant GABAArchiv der Pharmazie · 2026Article
- Effects of Chronic Administration of a Standardized Rice Bran Supplement on Sleep Architecture and Profiles in Mice: A Comparative Study with a Hypnotic Drug Zolpidem.Journal of microbiology and biotechnology · 2025Article
- Article
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5 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
aimZolpidem is a non-benzodiazepine agonist at benzodiazepine binding site in GABA(A) receptors, which is increasingly prescribed. Recent studies suggest that prolonged zolpidem treatment induces tolerance. The aim of this study was to explore the adaptive changes in GABA(A) receptors following short and long-term exposure to zolpidem in vitro.
methodsHuman embryonic kidney (HEK) 293 cells stably expressing recombinant α1β2γ2s GABA(A) receptors were exposed to zolpidem (1 and 10 μmol/L) for short-term (2 h daily for 1, 2, or 3 consecutive days) or long-term (continuously for 48 h). Radioligand binding studies were used to determine the parameters of [(3)H]flunitrazepam binding sites.
resultsA single (2 h) or repeated (2 h daily for 2 or 3 d) short-term exposure to zolpidem affected neither the maximum number of [(3)H]flunitrazepam binding sites nor the affinity. In both control and short-term zolpidem treated groups, addition of GABA (1 nmol/L-1 mmol/L) enhanced [(3)H]flunitrazepam binding in a concentration-dependent manner. The maximum enhancement of [(3)H]flunitrazepam binding in short-term zolpidem treated group was not significantly different from that in the control group. In contrast, long-term exposure to zolpidem resulted in significantly increase in the maximum number of [(3)H]flunitrazepam binding sites without changing the affinity. Furthermore, long-term exposure to zolpidem significantly decreased the ability of GABA to stimulate [(3)H]flunitrazepam binding.
conclusionThe results suggest that continuous, but not intermittent and short-term, zolpidem-exposure is able to induce adaptive changes in GABA(A) receptors that could be related to the development of tolerance and dependence.
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