Dynamics of histamine H(3) receptor antagonists on brain histamine metabolism: do all histamine H(3) receptor antagonists act at a single site?

  title={Dynamics of histamine H(3) receptor antagonists on brain histamine metabolism: do all histamine H(3) receptor antagonists act at a single site?},
  author={William G. Barnes and D L Boyd and Lindsay B. Hough},
  journal={European journal of pharmacology},
  volume={431 2},
Membrane‐bound histamine N‐methyltransferase in mouse brain: possible role in the synaptic inactivation of neuronal histamine
Functional evidence for the existence of membrane‐bound HNMT is demonstrated and the present work suggests that levels of biologically active histamine may be controlled by an extracellular process.
Assessment of pharmacology and potential anti-obesity properties of H3 receptor antagonists/inverse agonists
The goal of this review is to appraise findings and forecast whether any H3 antagonists/inverse agonists will provide clinical utility to treat human obesity.
Central H3R activation by thioperamide does not affect energy balance
Cognitive enhancing effects of drugs that target histamine receptors
New findings suggest important therapeutic roles for histamine and therapeutic potential for drugs that interdict the histaminergic pathways in various neurological diseases, particularly those having a cognitive deficit that these drugs may be anticipated to ameliorate.
Histamine H3 receptor as a drug discovery target.
The current medicinal chemistry programs are based on the monumental amount of research effort that has gone into establishing various aspects of H3 receptor biology, and suggest an abundance of therapeutic applications for small-molecule receptor modulators.
Roles of central histaminergic system in glucose metabolisms and food intake in sheep
In conclusion, the central histaminergic system is involved in the regulation of glucose metabolisms and food intake in ruminants.
New concepts of histamine receptors and actions
Investigation of other actions of histamine and the identification of H2, H3, and now H4 receptors have suddenly reignited the search for new mono- and multi-receptor-specific agonists and antagonists.
Perspectives on cognitive domains, H3 receptor ligands and neurological disease
  • A. Hancock, G. Fox
  • Biology, Psychology
    Expert opinion on investigational drugs
  • 2004
Histamine H3 receptor agonists and antagonists have been evaluated in numerous in vitro and in vivo animal models to better understand how H3 receptors modulate neurotransmitter function in the


Histamine turnover in regions of rat brain
Effects of the Histamine H3‐Agonist (R)‐α‐Methylhistamine and the Antagonist Thioperamide on Histamine Metabolism in the Mouse and Rat Brain
Results indicate that a potent and selective H3‐agonist, (R)‐α‐methylhistamine, and an H3-antagonist, thioperamide, have potent effects on HA turnover in vivo in the brain.
Inhibition of brain histamine metabolism by metoprine.
Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.