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1
The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.
PubMed Open HTML    
Connelly WM Chazot PL  » 
Br J Pharmacol (2009) Show Abstract »
In layer IV of the mouse somatosensory cortex, the H4 receptor agonist 4-methyl histamine (20 micromol x L(-1)) directly hyperpolarized neurons, an effect that was blocked by the selective H4 receptor antagonist JNJ 10191584, and promoted outwardly rectifying currents in these cells.
2
Furthermore, neuronal histamine release induced by thioperamide may suppress morphine-induced antinociception through H1 receptors.
3
Effects of drugs acting as histamine releasers or histamine receptor blockers on an experimental anxiety model in mice.
PubMed Open HTML    
Yuzurihara M Maruyama Y  » 
Pharmacol Biochem Behav (2000) Show Abstract »
These results suggest that not only neuronal histamine release induced by thioperamide but also non-neuronal (mast cells) histamine release induced by Compound 48/80 play an important role in inducing experimental anxiety via post-synaptic H(1) and H(2) receptors.
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4
These data suggest that thioperamide induces the release of neuronal histamine, which in turn stimulates both H1- and H2-receptors to produce the anxiogenic effect.
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5
Neuronal histamine in the hypothalamus suppresses food intake in rats.
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Ookuma K Fujimoto K  » 
Brain Res (1993) Show Abstract »
Conversely, thioperamide, which facilitates both synthesis and release of neuronal histamine by blocking presynaptic autoinhibitory H3 receptors, significantly decreased food intake after infusion of a 100-nmol dose into the third cerebroventricle.
6
Thioperamide, a histamine H3 receptor antagonist, increases GABA release from the rat hypothalamus.
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Yamamoto Y Yamatodani A  » 
Methods Find Exp Clin Pharmacol (1997) Show Abstract »
These 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.
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7
From this in vitro experiment, the conversion of N-telemethylhistamine to N-tele-methylimidazoleacetic acid may be inhibited by thioperamide, suggesting that thioperamide may affect the regulation of histamine metabolism within histaminergic neurons.
8
These results suggest that the thioperamide may have a specific effect on NPY receptor-mediated neuronal systems related to feeding.
9
Effects of the H3 receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions.
PubMed Open HTML    
Brabant C Tirelli E  » 
Psychopharmacology (Berl) (2008) Show Abstract »
Our data suggest that thioperamide, at least at 10 mg/kg, increases cocaine-induced locomotion through the combination of pharmacokinetic effects and the blockade of H3 receptors located on non-histaminergic neurons.
10
Finally, in KA-treated slices, the H3 receptor antagonist thioperamide enhanced the neuroprotective effect of histaminergic neurons, whereas the H1 receptor antagonists triprolidine and mepyramine dose-dependently decreased the neuroprotection in HI plus HY (POST).
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