Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Nα-methylhistamine
References (18)
- et al.
Eur. J. Pharmacol
(1987) - et al.
Eur. J. Pharmacol
(1989) - et al.
Life Sci
(1967) Anal. Biochem
(1976)- et al.
- et al.
Nature
(1987) - et al.
Neuroscience
(1987) - et al.
Nature
(1983) - et al.
NaunynSchmiedeberg's Arch. Pharmacol
(1988)
Cited by (86)
Histamine H <inf>3</inf> receptors modulate depolarization-evoked [ <sup>3</sup>H]-noradrenaline release from rat olfactory bulb slices
2012, NeuropharmacologyCitation Excerpt :N-α-[methyl-3H]-histamine (85.4 Ci/mmol), [ring-2,5,6-3H]-l-noradrenaline (44.6 Ci/mmol) and [3H]-dopamine (48 Ci/mmol) were from Perkin Elmer (Boston, MA, USA). Specific [3H]-NMHA binding yielded maximum binding (Bmax) 106 ± 19 fmol/mg protein (mean ± standard error, s.e.m.; 4 experiments, Fig. 1A) and equilibrium dissociation constant (Kd) 0.68 ± 0.11 nM, the latter in good agreement with values reported for rodent brain (0.4–0.71 nM; Kathmann et al., 1993; Korte et al., 1990; Nickel et al., 2001). Specific [3H]-NMHA binding was inhibited in a concentration-dependent manner by the selective H3R agonists immepip and (R)(−)-α-methylhistamine (RAMH) and the antagonist clobenpropit (Fig. 1B).
Pre-synaptic histamine H<inf>3</inf> receptors modulate glutamatergic transmission in rat globus pallidus
2011, NeuroscienceCitation Excerpt :Specific [3H]-NMHA binding to GP membranes yielded maximum binding (Bmax.) 162±29 fmol/mg protein (mean±standard error, SEM; four determinations, Fig. 1A) and equilibrium dissociation constant (Kd) 0.58±0.09 nM, the latter in good agreement with values reported for rodent brain (Korte et al., 1990; Kathmann et al., 1993; Nickel et al., 2001). The H3R agonist immepip and the antagonists clobenpropit, thioperamide and A-331440 inhibited in a concentration-dependent manner [3H]-NMHA binding (Fig. 1B).
Pre-synaptic histamine H<inf>3</inf> receptors regulate glutamate, but not GABA release in rat thalamus
2007, NeuropharmacologyCitation Excerpt :Specific [3H]-NMHA binding to membranes from rat thalamus synaptosomes (Fig. 1A) yielded maximum binding (Bmax) 141 ± 12 fmol/mg protein (four experiments). The estimate for the equilibrium dissociation constant (Kd) was 0.78 ± 0.20 nM, in good agreement with values reported for rat cerebral cortex (0.7 nM, Kathmann et al., 1993), mouse cerebral cortex (0.71 nM, Nickel et al., 2001) and guinea-pig brain (0.4 nM, Korte et al., 1990). [ 3H]-NMHA binding was inhibited in a concentration-dependent manner by histamine (Fig. 1B), with the curve fitting better to the two-site model (see Table 1 for pKi estimates).
Use 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 :Receptor-selective radioligands have been demonstrated to be useful tools in the characterization of many receptors (Bylund and Toews, 1993), including histamine H3 receptors. For example, selective agonist ligands [3H](R)-α-methyhistamine ([3H]RαMH) (West et al., 1990) and [3H](N)-α-methyhistamine ([3H]NαMH) (Korte et al., 1990) have been widely used in radioligand binding assays for studying receptor expression and pharmacology. However, agonist ligands may be able to label only the fraction of the total receptor pool that has high affinity for the agonist.
The Marine Bromotyrosine Derivatives
2005, Alkaloids: Chemistry and BiologyCitation Excerpt :The alkaloids were less active than 3’-azido-3’-deoxythymidine (AZT, ED50 0.10 μM), but were comparable to 2’,3’-dideoxycytidine (ddCyd ,ED50 15 μM) in these assays. Fistularin-3 (79) also exhibited anti-HIV-1 activity with an EC50 value of 6.9 μM (311) Reverse transcriptase (RT) plays a critical role in the early steps of the life of human immunodeficiency virus (HIV) (304), and for over a decade has been one of the major targets of AIDS therapy.
Identification of a dual histamine H<inf>1</inf>/H<inf>3</inf> receptor ligand based on the H<inf>1</inf> antagonist chlorpheniramine
2003, Bioorganic and Medicinal Chemistry Letters