Pre-synaptic histamine H3 receptors modulate glutamatergic transmission in rat globus pallidus

Osorio-Espinoza, Angélica; Alatorre, Alberto; Ramos-Jiménez, Judith; Garduño-Torres, Belén; Garcı́a-Ramı́rez, Martha; Querejeta, Enrique; Arias‐Montaño, José‐Antonio

doi:10.1016/j.neuroscience.2010.12.051

Cited by 18 publications

(23 citation statements)

References 72 publications

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“…This effect was accompanied by an increase in the fEPSP paired pulse ratio (Figure 2A), suggesting that methimepip reduced the probability of glutamate release in control rats. In agreement with this observation, several studies indicate a role for histamine H 3 receptors in modulating glutamate release in the medial frontal cortex (Welty and Shoblock, 2009), globus pallidus (Osorio-Espinoza et al, 2011), thalamus (Garduno-Torres et al, 2007), striatum (Molina-Hernandez et al, 2001) and dentate gyrus (Brown and Haas, 1999) of rats. Since no effects were observed in the PS paired-pulse ratio at stimulus intensities sufficient to elicit a large PS (Figure 3), it is not likely that the reductions in E-S coupling can be attributed to elevated GABA release.…”

Section: Discussionsupporting

confidence: 65%

Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Varaschin

Rosenberg

Hamilton

et al. 2014

Alcohol Clin Exp Res

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We previously reported that prenatal alcohol-induced deficits in dentate gyrus (DG) long-term potentiation (LTP) are ameliorated by the histamine H3 receptor inverse agonist ABT-239. ABT-239 did not enhance LTP in control rats, suggesting a heightened H3 receptor-mediated inhibition of glutamate release in prenatal alcohol-exposed (PAE) offspring. As the modulation of glutamate release is one important facet of LTP, we examined the effect of methimepip, a histamine H3 receptor agonist, on DG granule cell excitability, glutamate release and LTP in control and PAE rats. Long-Evans rat dams voluntarily consumed either a 0% or 5% ethanol solution four hours daily throughout gestation. Male adult offspring were anesthetized with urethane and electrodes implanted into the entorhinal cortex and DG. PAE reduced coupling of excitatory post-synaptic field potentials to population spikes, an effect mimicked in control rats treated with 1 mg/kg methimepip. Methimepip decreased release probability in controls but not in PAE offspring. GABAergic feedback inhibition of granule cell responsiveness was not affected by either PAE or methimepip. PAE reduced LTP in the DG, another effect mimicked in methimepip-treated control rats. Again, methimepip did not exacerbate the PAE-induced LTP deficit. Thus, while methimepip treatment of control rats mimicked some baseline and activity-dependent deficits observed in saline-treated PAE offspring, methimepip treatment of PAE rats did not exacerbate these deficits. Whether the absence of an added methimepip effect in PAE offspring is a consequence of a “floor effect” for the responses measured or is due to differential drug dose responsiveness will require further investigation. Further, more detailed studies of H3 receptor-mediated responses in vitro may provide clearer insights into the role of the H3 receptor regulation of excitatory transmission at the perforant path - DG synapse in PAE rats.

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Section: Discussionsupporting

confidence: 65%

Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Varaschin

Rosenberg

Hamilton

et al. 2014

Alcohol Clin Exp Res

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“…Histamine, a neurotransmitter, is involved in multiple physiological processes by coupling to four distinct, but related, G protein‐coupled receptors (GPCRs): H1Rs, H2Rs, H3Rs, and H4Rs . The involvement of histamine receptors (HRs) in the cognitive process has long been confirmed, especially in the case of H3Rs . The H3R is mainly expressed in nerve terminals, where it participates in the processes of memory and cognitive action .…”

Section: Introductionmentioning

confidence: 99%

Visualization of the activation of the histamine H3 receptor (H3R) using novel fluorescence resonance energy transfer biosensors and their potential application to the study of H3R pharmacology

et al. 2018

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Activation of the histamine-3 receptor (H3R) is involved in memory processes and cognitive action, while blocking H3R activation can slow the progression of neurological disorders, such as Alzheimer's disease, schizophrenia and narcolepsy. To date, however, no direct way to examine the activation of H3R has been utilized. Here, we describe a novel biosensor that can visualize the activation of H3R through an intramolecular fluorescence resonance energy transfer (FRET) signal. To achieve this, we constructed an intramolecular H3R FRET sensor with cyan fluorescent protein (CFP) attached at the C terminus and yellow fluorescent protein (YFP) inserted into the third intracellular loop. The sensor was found to internalize normally on agonist treatment. We measured FRET signals between the donor CFP and the acceptor YFP in living cells in real time, the results of which indicated that H3R agonist treatment (imetit or histamine) increases the FRET signal in a time- and concentration-dependent manner with Kon and Koff values consistent with published data and which maybe correlated with decreasing cAMP levels and the promotion of ERK1/2 phosphorylation. The FRET signal was inhibited by H3R antagonists, and the introduction of mutations at F419A, F423A, L426A and L427A, once again, the promotion of ERK1/2 phosphorylation, was diminished. Thus, we have built a H3R biosensor which can visualize the activation of receptor through real-time structure changes and which can obtain pharmacological kinetic data at the same time. The FRET signals may allow the sensor to become a useful tool for screening compounds and optimizing useful ligands.

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“…Histamine also exerts multiple modulatory roles in basal ganglia circuits . For example, it activates medium spiny neurons, presynaptically inhibits glutamate release from corticostriate and thalamostriatal terminals, modulates the effects of dopamine and adenosine, inhibits serotonergic and GABAergic transmission in the substantia nigra pars compacta, antagonizes adenosine 2A receptor effects on GABA release from striato‐pallidal projections, and inhibits glutamate release in the globus pallidus . These multiple actions may contribute to differences in the motor manifestation of MSA and PD .…”

Section: Discussionmentioning

confidence: 99%

Histaminergic tuberomammillary neuron loss in multiple system atrophy and dementia with Lewy bodies

et al. 2015

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Pre-synaptic histamine H3 receptors modulate glutamatergic transmission in rat globus pallidus

Cited by 18 publications

References 72 publications

Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Visualization of the activation of the histamine H3 receptor (H3R) using novel fluorescence resonance energy transfer biosensors and their potential application to the study of H3R pharmacology

Histaminergic tuberomammillary neuron loss in multiple system atrophy and dementia with Lewy bodies

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Pre-synaptic histamine H3 receptors modulate glutamatergic transmission in rat globus pallidus

Cited by 18 publications

References 72 publications

Differential Effects of the Histamine H3Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Differential Effects of the Histamine H3Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Visualization of the activation of the histamine H3 receptor (H3R) using novel fluorescence resonance energy transfer biosensors and their potential application to the study of H3R pharmacology

Histaminergic tuberomammillary neuron loss in multiple system atrophy and dementia with Lewy bodies

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Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats

Differential Effects of the Histamine H₃Receptor Agonist Methimepip on Dentate Granule Cell Excitability, Paired-Pulse Plasticity and Long-Term Potentiation in Prenatal Alcohol-Exposed Rats