Effects of selected histamine H3 receptor antagonists on tele-methylhistamine levels in rat cerebral cortex.

@article{Yates1999EffectsOS,
  title={Effects of selected histamine H3 receptor antagonists on tele-methylhistamine levels in rat cerebral cortex.},
  author={Stephen L. Yates and Clark E. Tedford and Rosilyn Gregory and Gary Pawlowski and Michael Handley and D L Boyd and Lindsay B. Hough},
  journal={Biochemical pharmacology},
  year={1999},
  volume={57 9},
  pages={
          1059-66
        }
}
Regulation of Norepinephrine Release from Isolated Bovine Irides by Histamine
TLDR
It is concluded that histamine produces an inhibitory action on sympathetic neurotransmission in the bovine iris, an effect mimicked by selective H3-receptor agonists and blocked by H3 -antagonists.
Simultaneous quantitation of histamine and its major metabolite 1-methylhistamine in brain dialysates by using precolumn derivatization prior to HILIC-MS/MS analysis
TLDR
This method provided the required selectivity, sensitivity, accuracy, and precision to assess release kinetics of histamine and 1-methylhistamine in several hundred rat brain microdialysates after intravenous infusion of CNS drug candidates.
Histamine H3 receptor as a drug discovery target.
TLDR
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.
High constitutive activity of native H3 receptors regulates histamine neurons in brain
TLDR
It is shown that constitutive activity of native H3 receptors is present in rodent brain and that it controls histaminergic neuron activity in vivo, and inverse agonists may find therapeutic applications, even in the case of diseases involving non-mutated receptors expressed at normal levels.
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
TLDR
The terminal nitrogen atom of histamines was modified with lipophilic substituents to investigate the structure-activity relationship of histamine type 3 receptor (H3R) agonists, with the most potent compound, 4-(2-(4-tert-butylphenylthio)ethyl)-1H-imidazole, possessing in vivo agonistic activity.
...
...

References

SHOWING 1-10 OF 26 REFERENCES
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
TLDR
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.
Thioperamide, a histamine H3 receptor antagonist, increases GABA release from the rat hypothalamus.
TLDR
The results suggest that the effect of thioperamide on GABA release is not mediated by histamine H3 receptors and that thiOPERamide acts on the transporter to cause an efflux of GABA from neurons and/or glia.
Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor
TLDR
It is shown here that histamine inhibits its own release from depolarized slices of rat cerebral cortex, an action apparently mediated by a class of receptor (H3) pharmacologically distinct from those previously characterized, that is, the H1 and H2 receptors.
Search for novel leads for histamine H3-receptor antagonists: oxygen-containing derivatives.
TLDR
The most potent compounds in vitro and in vivo also showed high H3-receptor selectivity when tested at other histamine receptor subtypes, and some of these novel antagonists are useful tools for investigations on ligand-recept interaction because of their distinct receptor activities.
An improved GCMS method to measure tele-methylhistamine.
Characterization of Basal and Morphine‐Induced Histamine Release in the Rat Periaqueductal Gray
TLDR
Results suggest that basal and morphine‐induced HA release in the rat PAG have a neuronal origin, and antinociceptive doses of systemic morphine are shown to increase extracellular histamine levels in the PAG.
...
...