Stereoselectivity of the histamine H3-presynaptic autoreceptor
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Cited by (55)
Cherry-picked ligands at histamine receptor subtypes
2016, NeuropharmacologyCitation Excerpt :The methylated analog 3H-Nα-methylhistamine (NAMH, 30) (Arrang et al., 1987) is not selective for H3R (vs H1R, H2R), but has found a wide use in radioligand competition binding assays due to its high affinity at rat H3Rs (Arrang et al., 1983; Hill et al., 1997) and ready availability in tritiated form. R-(α)-methylhistamine (28) is highly potent (Arrang et al., 1985a, 1985b; Hill et al., 1997) and is also used as an in vitro agonist tool (Fig. 5). Also, R-(α)-methylhistamine does have significant H4R activity (Liu et al., 2001; Morse et al., 2001; Panula et al., 2015).
Neuronal histamine and cognitive symptoms in Alzheimer's disease
2016, NeuropharmacologyCitation Excerpt :While the H1R and H2R are post- and extra-synaptic receptors (Mizuguchi et al., 1991), the H3R can act also as an autoreceptor on histaminergic axon terminals, where it modulates histamine release and turnover via feedback inhibition of histamine synthesis. It can also function as a heteroreceptor, when it is located at non-histaminergic fibers (Arrang et al., 1985; Gbahou et al., 2012). Here, the stimulation of the H3R can inhibit the synthesis and release of various other neurotransmitters including GABA, dopamine, serotonin and acetylcholine.
New high affinity H<inf>3</inf> receptor agonists without a basic side chain
2005, Bioorganic and Medicinal ChemistryH<inf>3</inf> histamine receptors: The gene knockout data so far
2004, Current Anaesthesia and Critical Care6 The Histamine H<inf>3</inf> Receptor and its Ligands
2001, Progress in Medicinal ChemistrySelective ligands as tools to study histamine receptors
2000, European Journal of Medicinal Chemistry