European Journal of Pharmacology: Molecular Pharmacology
Histamine H3 receptor binding sites in rat brain membranes: modulations by guanine nucleotides and divalent cations
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Identification of histaminergic neurons through histamine 3 receptor-mediated autoinhibition
2016, NeuropharmacologyCitation Excerpt :Histaminergic neurons express only one type of histamine receptors, the autoinhibitory H3R. The H3R restricts the influx of Ca2+, which is essential for histamine release (Arrang et al., 1985, 1990). H3R activation suppresses voltage-activated calcium channels in histaminergic neurons explaining the inhibition of histamine release and spontaneous firing (Stevens and Haas, 1996; Stevens et al., 2001; Takeshita et al., 1998).
Identification and pharmacological characterization of the histamine H <inf>3</inf> receptor in cultured rat astrocytes
2013, European Journal of PharmacologyCitation Excerpt :Due to low expression of native histamine H3 receptor in our model of astrocytes low Bmax was expected and can not be compared with Bmax in other model systems. [ 3H]NαMH as a selective agonist recognizes both high- and low-affinity receptor binding sites (Arrang et al., 1990; West et al., 1990; Witte et al., 2006). In our study we obtained no compelling evidence for [3H]NαMH to bind two classes of histamine H3 receptor sites since accurate estimation of low-affinity binding parameters was not possible and, in addition, Schatchard plot was linear and Hill slope was near unity.
Seeking a mechanism of action for the novel anticonvulsant lacosamide
2006, NeuropharmacologyUse of an inverse agonist radioligand [<sup>3</sup>H]A-317920 reveals distinct pharmacological profiles of the rat histamine H<inf>3</inf> receptor
2006, NeuropharmacologyCitation Excerpt :However, agonist ligands may be able to label only the fraction of the total receptor pool that has high affinity for the agonist. Moreover, affinities of agonist radioligands are often highly dependent upon the presence or absence of guanine nucleotides or various ions in the assay buffer (Motulsky and Insel, 1983; Arrang et al., 1990; Kilpatrick and Michel, 1991). H3 receptor antagonist radioligands have also been used to define H3 receptor pharmacology.