Characterization of metabotropic glutamate receptors in rat C6 glioma cells

European Journal of Pharmacology
J L AlbasanzM Martín

Abstract

Metabotropic glutamate receptors in rat C6 glioma cells have been characterized by pharmacological and kinetic binding experiments, using both L-[3H]glutamate and [3H(+/-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid ([3H](+/-)-trans-ACPD) radioligands. Saturation experiments revealed a single binding site with a Kd = 1250 +/- 101 nM and Bmax = 12.1 +/- 1.8 pmol/mg protein when the assays were performed with L-[3H]glutamate as radioligand in the presence of AMPA, kainate, NMDA and DL-threo-beta-hydroxyaspartic acid. When [3H](+/-)-trans-ACPD was used as radioligand, the kinetic parameters obtained were Kd = 2605 +/- 1042 nM and Bmax = 13.66 +/- 5.01 pmol/mg protein. Pharmacological characterization indicated that specific binding of L-[3H]glutamate was sensitive to different agonists of mGlu receptors, showing a rank order of affinity L-glutamate > L-quisqualic acid > (+/-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid (trans-ACPD) > ibotenic acid > (2S, 'S,2'S)-2-(carboxycyclopropyl)glycine (L-CCG-I). Specific binding of L-[3H]glutamate to mGlu receptors is regulated by guanine nucleotides. Guanylyl imidodiphosphate (Gpp(NH)p) causes an affinity shift on the L-glutamate dose-response curve, increasing the IC50 value. Thes...Continue Reading

References

Jan 1, 1992·Neuron·Y TanabeS Nakanishi
Apr 10, 1992·European Journal of Pharmacology·O ManzoniJ Bockaert
Nov 1, 1992·Proceedings of the National Academy of Sciences of the United States of America·J P PinS F Heinemann
Jul 12, 1991·European Journal of Pharmacology·M MartínA Cubero
Dec 1, 1990·Trends in Pharmacological Sciences·D SchoeppF Sladeczek
Jan 1, 1990·Annual Review of Pharmacology and Toxicology·L Birnbaumer
Jul 1, 1990·Trends in Pharmacological Sciences·G L Collingridge, W Singer
Sep 1, 1990·Trends in Pharmacological Sciences·B Meldrum, J Garthwaite
Aug 3, 1989·European Journal of Pharmacology·E PalmerC W Cotman
Jan 1, 1987·Annual Review of Biochemistry·A G Gilman
Jan 1, 1984·Journal of Neurochemistry·F Fonnum
Jan 1, 1995·Neuropharmacology·J P Pin, R Duvoisin
May 1, 1994·Neurochemistry International·D D Schoepp
Jan 1, 1993·Trends in Pharmacological Sciences·D D Schoepp, P J Conn
Mar 30, 1994·Biochemical and Biophysical Research Communications·R MinakamiH Sugiyama
Jan 1, 1994·Annual Review of Biophysics and Biomolecular Structure·S Nakanishi, M Masu
Jan 1, 1994·Annual Review of Neuroscience·M Hollmann, S Heinemann
Jun 1, 1993·Trends in Pharmacological Sciences·G Milligan
Jan 7, 1993·Nature·T V Bliss, G L Collingridge
Nov 10, 2010·Journal of Receptor and Signal Transduction Research·Werner Schlegel

❮ Previous
Next ❯

Citations

Jul 12, 2002·Journal of Neuroscience Research·Tomasz KockiJan Albrecht
Mar 1, 2002·Brain Research. Molecular Brain Research·José Luis AlbasanzMairena Martín
May 17, 2000·Neurochemistry International·L BuzańskaJ Albrecht
Mar 13, 2014·Journal of Neural Transmission·Andrzej StepulakChrysanthy Ikonomidou
Mar 24, 2010·Neurochemical Research·Carlos Alberto CastilloJosé Luis Albasanz
Aug 7, 2009·Cell Calcium·Elke De VuystLuc Leybaert
Aug 30, 2008·Progress in Neuro-psychopharmacology & Biological Psychiatry·Kyungsoo RohSeok Hyeon Kim
Jun 17, 2008·Neuropharmacology·Seung-Shick ShinSuzie Chen
May 12, 2007·Brain Research·Inmaculada IglesiasMairena Martín
Jul 15, 2015·Molecular and Cellular Neurosciences·Rafael Andrés Posada-DuqueGloria Patricia Cardona-Gómez
Jun 14, 2005·Neurological Research·Gelsomina De StasioRoberto Pallini
Jan 19, 2007·Journal of Neurochemistry·Mary J Clark, John R Traynor
Apr 9, 2015·Frontiers in Cellular Neuroscience·Aristeidis A KritisTheofanis D Vavilis
Jun 14, 2003·The Journal of Biological Chemistry·Deepika RajeshSteven P Howard

❮ 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.