In vivo occupancy of histamine H3 receptors by thioperamide and (R)-α-methylhistamine measured using histamine turnover and an ex vivo labeling technique
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Cited by (39)
Modulation of behavior by the histaminergic system: Lessons from HDC-, H<inf>3</inf>R- and H<inf>4</inf>R-deficient mice
2014, Neuroscience and Biobehavioral ReviewsCitation Excerpt :Moreover, a certain degree of BBB penetration after intravenous or i.p. administration was demonstrated for both RAMH (Taylor et al., 1992; Yamasaki et al., 1994) and thioperamide (Taylor et al., 1992). This was determined by fluorescence-spectroscopy-coupled high-performance liquid chromatography (HPLC) (Yamasaki et al., 1994) or by determination of histamine turnover in the cortex (Taylor et al., 1992) or ex vivo [3H]RAMH binding (Taylor et al., 1992). Administration of the HDC-inhibitor α-fluoromethylhistamine (α-FMH) increased food intake, but did not influence the anorexigenic effect of imetit (Yoshimoto et al., 2006a).
In vivo receptor occupancy assay of histamine H <inf>3</inf> receptor antagonist in rats using non-radiolabeled tracer
2012, Journal of Pharmacological and Toxicological MethodsCitation Excerpt :H3R antagonists are reported to be effective in cognition enhancement at a moderate level of occupancy and robust wake promoting activity at higher levels of occupancy (Le et al., 2008). In preclinical research, radiolabeled ligands are being commonly employed to measure the brain H3R occupancy by ex vivo or in vivo binding methods (Le et al., 2008; Ligneau, Lin, & Vanni-Mercier, 1998; Medhurst, Briggs, et al., 2007; Miller et al., 2009; Stephen et al., 1999; Taylor, Michel, & Kilpatrick, 1992). During ex vivo method, the test compound treated animals are sacrificed to excise the brain tissues and radioligand competition binding is carried out under in-vitro condition.
Target site occupancy: Emerging generalizations from clinical and preclinical studies
2009, Pharmacology and TherapeuticsStructurally novel histamine H<inf>3</inf> receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats
2007, Biochemical PharmacologyCitation Excerpt :From GTPγS binding studies, pIC50 values were generated from dose–response curves using Grafit 5.0.8 (Erithacus Software Ltd.). Ex vivo binding studies were carried out based on methodology previously reported [49,52]. Adult male rats (Lister hooded 200–250 g, Charles River, UK) received vehicle (1%, w/v aqueous methylcellulose), GSK207040 (0.01, 0.03, 0.1, 0.3, 1 or 3 mg/kg) or GSK334429 (0.03, 0.1, 0.3, 1, 3 and 10 mg/kg) by oral gavage (n = 3 per group) and were sacrificed 2 or 3 h later.
Role of the histamine system in nefopam-induced antinociception in mice
2004, European Journal of Pharmacology