PMID: 6113878Jul 20, 1981Paper

Dihydropicrotoxinin binding sites in mammalian brain: interaction with convulsant and depressant benzodiazepines

Brain Research
F Leeb-LundbergR W Olsen

Abstract

The specific binding of [3H] alpha-dihydropicrotoxinin to rat brain membranes was inhibited competitively and potently (IC50 congruent to 100 nM) by a convulsant benzodiazepine drug, RO5-3663. This compound did not inhibit high affinity flunitrazepam binding to the same tissue under similar conditions, and its reported pharmacological activity as an antagonist of GABAergic synaptic transmission, which resembles that of picrotoxinin, appears to involve the picrotoxinin binding sites. Other benzodiazepines such as diazepam, in micromolar concentrations, inhibited picrotoxinin binding in a stereospecific and chemically specific manner. However, the order of potency of a series of depressant benzodiazepines did not correlate well with pharmacological activities nor with reported activities for displacement of high affinity benzodiazepine 'receptor' binding sites (although heterogeneity of both picrotoxinin and benzodiazepine binding site populations may make difficult such comparisons). A comparison of benzodiazepine-displaceable benzodiazepine binding and benzodiazepine-displaceable picrotoxinin binding for different brain regions and subcellular fractions revealed a very similar though not identical distribution of these two clas...Continue Reading

References

May 1, 1979·Pharmacology, Biochemistry, and Behavior·R F SquiresB Beer
Sep 15, 1979·Biochemical Pharmacology·P R Andrews, G A Johnston
Mar 1, 1979·Journal of Neurochemistry·P J Syapin, P Skolnick
Mar 1, 1979·Neuropharmacology·M K Ticku, R W Olsen
Nov 23, 1979·European Journal of Pharmacology·P Supavilai, M Karobath
May 8, 1978·Life Sciences·D V GreenleeR W Olsen
Apr 21, 1977·Nature·R F Squires, C Brastrup
Jan 18, 1980·Science·J F TallmanD W Gallager
Apr 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·C BraestrupC E Olsen
Jul 11, 1980·European Journal of Pharmacology·P SkolnickJ L Barker
Jul 17, 1980·Nature·W Sieghart, M Karobath
Dec 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·F Leeb-LundbergR W Olsen
Jul 1, 1980·Neuroscience Letters·M Willow, G A Johnston
Jul 11, 1980·European Journal of Pharmacology·R W Olsen, F Leeb-Lundberg
Sep 15, 1980·Life Sciences·C NapiasR W Olsen

❮ Previous
Next ❯

Citations

Oct 1, 1982·Naunyn-Schmiedeberg's Archives of Pharmacology·L TurskiK H Sontag
Jul 1, 1985·Neurochemical Research·A Y ChwehH H Wolf
Jan 28, 1983·European Journal of Pharmacology·N L Harrison, M A Simmonds
Jul 16, 1984·Life Sciences·S Pellow, S E File
Nov 18, 1985·Life Sciences·R L Garrett, W M Bourn
Mar 1, 1989·Pharmacology, Biochemistry, and Behavior·M J Durcan, R G Lister
Feb 1, 1989·Pharmacology, Biochemistry, and Behavior·J A Griffith, D E Woolley
Jan 1, 1984·Neuroscience and Biobehavioral Reviews·S Pellow, S E File
Jan 1, 1985·Neuroscience and Biobehavioral Reviews·S J Cooper, L B Estall
Jan 1, 1985·Neuroscience and Biobehavioral Reviews·S Pellow
Jan 1, 1982·Progress in Neurobiology·J A Richter, J R Holtman
Dec 1, 1984·Pharmacology, Biochemistry, and Behavior·S V Vellucci, R A Webster
Jul 1, 1981·Journal of Neurochemistry·R W Olsen
Jan 1, 1988·British Journal of Pharmacology·R G Lister, D J Nutt

❮ 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.