A comparison of the pharmacological properties of recombinant human and rat alpha(1)beta(2)gamma(2L) GABA(A) receptors in Xenopus oocytes

Clinical and Experimental Pharmacology & Physiology
Mozibur RahmanMing-De Wang

Abstract

In the present study, we compared the pharmacology, particularly neurosteroid modulation of the GABA(A) receptor, between human and rat alpha(1)beta(2)gamma(2)(L) GABA(A) receptors and between human receptors containing the long (L) and short (S) forms of the gamma(2)-subunit. We observed that maximum responses to GABA were significantly higher with the human alpha(1)beta(2)gamma(2)(L) receptor compared with the rat receptor. In terms of neurosteroid modulation, increases in the EC(15) response to GABA induced by 3alpha-OH-5beta-pregnan-20-one (3alpha5betaP), 5alpha-androstane-3alpha,17beta-diol (3alpha5alphaADL) and 5alpha-pregnane-3alpha,20beta-diol (3alpha5alpha-diol) were significantly greater for the rat compared with the human receptor. Responses to 30 micromol/L GABA were inhibited by 3beta-OH-5alpha-pregnan-20-one (UC1010) and 5beta-pregnan-3beta,20(R)-diol (UC1020) to a greater degree for human and rat receptors, respectively. Responses to GABA + 3alpha5alphaTHDOC were inhibited by 5alpha-pregnan-3beta,20(S)-diol (UC1019) and pregnenolone sulphate to a greater degree for human and rat receptors, respectively. The GABA dose-response curves for human alpha(1)beta(2)gamma(2)(S) and alpha(1)beta(2)gamma(2)(L) receptors wer...Continue Reading

References

Dec 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·P WhitingL L Iversen
Sep 1, 1986·Journal of Steroid Biochemistry·A Lanthier, V V Patwardhan
Oct 1, 1994·Journal of Neurochemistry·Z U KhanA L De Blas
Jan 1, 1996·Neuropharmacology·D BelelliN C Lan
Aug 22, 1997·Brain Research·C CorpéchotJ P Fry
Jul 1, 1997·The Journal of Steroid Biochemistry and Molecular Biology·M D WangT Bäckström
May 15, 1998·Nature·K T Britton, G F Koob
Feb 9, 2000·Frontiers in Neuroendocrinology·N A Compagnone, S H Mellon
Apr 20, 2000·Neuroscience Research·K TsutsuiM Takase
Jul 7, 2001·Epilepsia·J Bauer
Jul 10, 2001·Epilepsia·D S ReddyM A Rogawski
Oct 16, 2001·International Review of Neurobiology·M WangM Bixo
Apr 17, 2002·Brain Research·Inga Maj JohanssonTorbjörn Bäckström
Aug 14, 2002·Pharmacotherapy·Richard G Wenzel, Carrie A Sarvis
Sep 6, 2002·Journal of Alzheimer's Disease : JAD·D B DubalP M Wise
Nov 12, 2003·Hormones and Behavior·Klaus A MiczekJoseph F De Bold
Mar 3, 2004·Annals of the New York Academy of Sciences·Torbjörn BäckströmElisabeth Zingmark
Dec 16, 2005·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Gustav AkkSteven Mennerick
Dec 20, 2005·Psychopharmacology·Anna-Carin N-WihlbäckTorbjörn Bäckström
Dec 22, 2005·Current Opinion in Pharmacology·Keith A Wafford, Bjarke Ebert
May 9, 2006·Hormones and Behavior·Magnus LöfgrenTorbjörn Bäckström
May 25, 2006·The Journal of Clinical Endocrinology and Metabolism·Helena HavlíkováLuboslav Stárka
Jun 15, 2007·Pharmacology & Therapeutics·Alastair M HosieTrevor G Smart

❮ Previous
Next ❯

Citations

Aug 31, 2001·Pharmacology, Biochemistry, and Behavior·S I WikinskiM C Rubio
Feb 21, 2013·Journal of Medicinal Chemistry·Barbora SlavíkováAlexander Kasal

❮ 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.