Central H3R activation by thioperamide does not affect energy balance

Pharmacology, Biochemistry, and Behavior
Dana K SindelarRobert Gadski

Abstract

The central histamine 3 receptor (H3R) is a presynaptic autoreceptor that regulates neuronal release and synthesis of histamine, and is thought to play a key role in controlling numerous central nervous system (CNS)-mediated parameters, including energy homeostasis. Thioperamide, the prototypical selective H3R antagonist, was used to examine the role that H3R plays in regulating energy balance in vivo. Thioperamide was administered either intraperitoneally or orally to rats and the pharmacokinetic parameters were examined along with central H3R binding and histaminergic system activation. Food intake and metabolic parameters of either route of thioperamide administration were likewise examined. In a dose-dependent manner, both the intraperitoneal and oral route of administration resulted in similar ex vivo binding curves and tele-methylhistamine dose-response curves despite the route of administration. However, only intraperitoneal administration of 30 mg/kg thioperamide resulted in a significant decrease in 24-h food intake (60% lower than control) and respiratory quotient (RQ), while the oral route of delivery did not. Moreover, the decrease in RQ with the 30 mg/kg ip administration also decreased energy expenditure (EE) thus...Continue Reading

References

Aug 2, 1990·European Journal of Pharmacology·R OishiK Saeki
Dec 1, 1989·Journal of Neurochemistry·M GarbargC Gros
Sep 1, 1988·Pharmacology, Biochemistry, and Behavior·N Orthen-Gambill
Aug 1, 1995·Pharmacology, Biochemistry, and Behavior·T Naruse, R Ishii
Sep 1, 1993·Physiology & Behavior·H YoshimatsuT Sakata
Dec 22, 1999·Physiology & Behavior·T MorimotoA Yamatodani
Jun 16, 2000·Brain Research·T MorimotoA Yamatodani
Dec 19, 2000·Biochemical and Biophysical Research Communications·T NakamuraK Tanaka
Dec 19, 2002·The Journal of Clinical Investigation·Kazuhiko TakahashiHidehito Kotani

❮ Previous
Next ❯

Citations

Jan 25, 2005·Nature Reviews. Drug Discovery·Rob LeursIwan J P de Esch
Sep 7, 2006·Proceedings of the National Academy of Sciences of the United States of America·Ryo YoshimotoShigeru Tokita
Apr 19, 2005·Expert Opinion on Investigational Drugs·Arthur A Hancock, Michael E Brune
Aug 8, 2014·Neuroscience and Biobehavioral Reviews·Erich H SchneiderRoland Seifert
Nov 27, 2007·European Journal of Pharmacology·Ryo YoshimotoShigeru Tokita
Jul 15, 2015·Neuropharmacology·Gustavo ProvensiMaria Beatrice Passani
Jun 28, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Alessandro PiniArianna Carolina Rosa
Sep 10, 2005·International Journal of Obesity : Journal of the International Association for the Study of Obesity·K MalmlöfK Rimvall
Jul 5, 2019·CNS & Neurological Disorders Drug Targets·Néstor F DíazAnayansi Molina-Hernández

❮ 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.