PMID: 8614277Jan 1, 1996Paper

Characterization and distribution of binding sites for [3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain

Life Sciences
M Rinaldi-CarmonaG Le Fur

Abstract

SR 141716A belongs to a new class of compounds (diarylpyrazole) that inhibits brain cannabinoid receptors (CB1) in vitro and in vivo. The present study showed that [3H]-SR 141716A binds with high affinity (Kd=0.61 +/- 0.06 nM) to a homogenous population of binding sites (Bmax=0.72 +/- 0.05 pmol/mg of protein) in rate whole brain (minus cerebellum) synaptosomes. This specific binding was displaced by known cannabinoid receptor ligands with the following rank order of potency SR 141716A > CP 55,940 > WIN 55212-2 = delta9-THC > anandamide. Apart from anandamide, all these compounds were found to interact competitively with the binding sites labeled by [3H]-SR 141716A. On the other hand, agents lacking affinity for cannabinoid receptors were unable to displace [3H]-SR 141716A from its binding sites (IC50 > 10 microM). In addition, the binding of [3H]-SR 141716A was insensitive to guanyl nucleotides. Regional rat brain distribution of CB1 cannabinoid receptors detected by [3H]-SR 141716A saturation binding and autoradiographic studies, showed that this distribution was very similar to that found for [3H]-CP 55,940. In vivo, the [3H]-SR 141716A binding was displaced by SR 141716A with ED50 values of 0.39 +/- 0.07 and 1.43 +/- 0.29 mg...Continue Reading

Citations

Nov 14, 1997·Clinical Reviews in Allergy & Immunology·B E Van Hoozen, C E Cross
Jun 7, 2005·Pharmacology, Biochemistry, and Behavior·Liana FattoreWalter Fratta
Jun 5, 1999·European Journal of Pharmacology·Z K KrowickiP J Hornby
Jan 1, 1997·Pharmacology & Therapeutics·R G Pertwee
Oct 6, 2001·Veterinary Immunology and Immunopathology·W PontiD Parolaro
Sep 18, 2002·Nuclear Medicine and Biology·William B MathewsRobert F Dannals
May 23, 2006·Nature Medicine·Fatima Teixeira-ClercSophie Lotersztajn
Feb 19, 2010·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Lene MartiniJennifer L Whistler
May 14, 1999·British Journal of Pharmacology·G GriffinM E Abood
Dec 5, 2000·Behavioural Pharmacology·B Scatton, D J Sanger
Feb 1, 1997·The European Journal of Neuroscience·M GlassY P Maneuf
Oct 16, 2014·Nature Reviews. Neuroscience·Raphael MechoulamAllyn C Howlett
Sep 21, 2010·European Journal of Pharmacology·Todd M SuterChristian C Felder
Jul 9, 2010·Fundamental & Clinical Pharmacology·Marie WennerbergGeorges Vauquelin
May 19, 2004·British Journal of Pharmacology·Saoirse E O'SullivanMichael D Randall
Jan 7, 2004·British Journal of Pharmacology·James D LeggettD A Kendall
Aug 17, 2004·British Journal of Pharmacology·Allyn C Howlett
Feb 6, 2004·British Journal of Pharmacology·Lisa Walter, Nephi Stella
Aug 23, 2007·Chemistry & Biodiversity·Eric Stern, Didier M Lambert
Aug 26, 2009·Fundamental & Clinical Pharmacology·M WennerbergGeorges Vauquelin
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
Aug 10, 2015·Toxicology in Vitro : an International Journal Published in Association with BIBRA·A OrtegaS A Del Angel
Feb 15, 2007·Expert Opinion on Therapeutic Targets·Ariane MallatSophie Lotersztajn
Jul 19, 2011·Neurochemistry International·Kathleen M BissetRussell A Nicholson
Jun 8, 2002·Prostaglandins, Leukotrienes, and Essential Fatty Acids·A H LichtmanB R Martin

❮ 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.