Differential effects of short- and long-term zolpidem treatment on recombinant α1β2γ2s subtype of GABA(A) receptors in vitro.

Aim: Zolpidem 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.

The effects of zolpidem treatment on GABA(A) receptors in cultured cerebellar granule cells: changes in functional coupling.

Aims: Hypnotic zolpidem is a positive allosteric modulator of γ-aminobutyric acid (GABA) action, with preferential although not exclusive binding for α1 subunit-containing GABA(A) receptors. The pharmacological profile of this drug is different from that of classical benzodiazepines, although it acts through benzodiazepine binding sites at GABA(A) receptors. The aim of this study was to further explore the molecular mechanisms of GABA(A) receptor induction by zolpidem.

Modulation of recombinant GABA(A) receptors by neurosteroid dehydroepiandrosterone sulfate.

Aim: To investigate whether long-term exposure to the neurosteroid dehydroepiandrosterone sulfate (DHEAS) induces adaptive changes of GABA(A) receptors related to the development of tolerance and dependence.

Methods: We compared the parameters of [(3)H]DHEAS binding and the effects of DHEAS on [(3)H]flunitrazepam binding in the membranes of HEK 293 cells, nontransfected or stably transfected with recombinant α(1)β(2)γ(2S) GABA(A) receptors. In HEK 293 cells expressing α(1)β(2)γ(2S) GABA(A) receptors, we investigated the effects of long-term DHEAS treatment on the [(3)H]flunitrazepam and [(3)H]t-butylbicycloorthobenzoate ([(3)H]TBOB) binding and on their modulation with GABA.

The effects of zolpidem treatment and withdrawal on the in vitro expression of recombinant alpha1beta2gamma2s GABA(A) receptors expressed in HEK 293 cells.

Zolpidem, a widely used hypnotic drug which acts through benzodiazepine binding sites, is a positive allosteric modulator of gamma-aminobutyric acid (GABA) action with preferential affinity for GABA(A) receptors containing alpha1 subunit. The pharmacological profile of zolpidem is different from that of classical benzodiazepines. The aim of this study was to find out whether zolpidem treatment triggers adaptive changes in the recombinant alpha1 subunit-containing GABA(A) receptors other than those observed following treatment with classical benzodiazepine-diazepam.

Zolpidem is a potent anticonvulsant in adult and aged mice.

Zolpidem is a widely used hypnotic drug acting via benzodiazepine binding sites on GABA(A) receptors. Several studies suggested that zolpidem might have better anticonvulsant potency than previously thought. To compare the sedative and anticonvulsant potency of this drug, we studied in male mice the influence of zolpidem (0.