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

Naunyn-Schmiedeberg's Archives of Pharmacology
Josipa VlainićD Pericić

Abstract

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. Radioligand binding studies showed that 2-day exposure of human embryonic kidney (HEK) 293 cells stably expressing recombinant alpha1beta2gamma2s GABA(A) receptors to zolpidem (10 muM) up-regulated the maximum number (B (max)) of [(3)H]flunitrazepam, [(3)H]muscimol, and [(3)H]t-butylbicycloorthobenzoate ([(3)H]TBOB) binding sites without changing their affinity (K (d)), suggesting an increase in total GABA(A) receptor number. Semi-quantitative RT-PCR analysis demonstrated increased levels of alpha1 subunit mRNA, while Western blot demonstrated up-regulated gamma2 subunit proteins, suggesting that zolpidem induced de novo synthesis of receptors proteins, at both the t...Continue Reading

References

Sep 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·S ArbillaS Z Langer
Apr 1, 1996·Trends in Neurosciences·R M McKernan, P J Whiting
May 1, 1996·Trends in Pharmacological Sciences·E Costa, A Guidotti
Jun 25, 1997·European Journal of Pharmacology·R A HoltI L Martin
Aug 5, 1997·Proceedings of the National Academy of Sciences of the United States of America·A Buhr, E Sigel
Aug 1, 1997·Brain Research. Molecular Brain Research·R A HoltA N Bateson
Nov 23, 2000·British Journal of Pharmacology·F CrestaniU Rudolph
Jan 29, 2002·Current Pharmaceutical Design·A N Bateson
Apr 23, 2002·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Gerry ShawFrank L Graham
Jul 20, 2002·Progress in Neurobiology·Esa R KorpiHartmut Lüddens
Sep 17, 2002·European Journal of Pharmacology·Enrico SannaGiovanni Biggio
Jan 22, 2005·Current Opinion in Pharmacology·Keith A Wafford
Jan 28, 2006·Pharmacology, Biochemistry, and Behavior·Jeanne M FaheyDavid J Greenblatt
Jan 25, 2008·Journal of Neural Transmission·Danka PericićDubravka Svob Strac
Nov 17, 2009·Brain Research·Josipa Vlainić, Danka Pericić
Feb 4, 2010·Pharmacological Reviews·Mikko Uusi-Oukari, Esa R Korpi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.