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Pharmacological characterisation of the histamine H3 receptor in the rat hippocampus
Brain Research, 1998The purpose of this report was to pharmacologically characterise the histamine H3 in the rat hippocampus using radioligand binding studies with the H3 receptor antagonist [125I]iodophenpropit and the H3 receptor mediated inhibition of [3H]noradrenaline release.
Henk Timmerman +5 more
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Biochemical properties of the histamine H3 receptor
1998Publisher Summary This chapter discusses biochemical properties of the histamine H 3 receptor and potential strategies that may end in the cloning of the H 3 receptor cDNA. From radioligand binding studies in which guanyl-nucleotids have been shown to inhibit the binding of H 3 agonists to the H 3 receptor, the interaction with a G-protein is ...
Henk Timmermann +2 more
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5 Recent Medicinal Chemistry of the Histamine H3 Receptor
2006Publisher Summary Following the cloning of the histamine H3 receptor cDNA, the level of activity amongst both academic and pharmaceutical company laboratories has increased enormously. This activity has provided a greater understanding of the basic biology of the target, answering many questions about the potential therapeutic roles for histamine H3 ...
Nicholas I. Carruthers +3 more
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Identification of two H3-histamine receptor subtypes.
Molecular Pharmacology, 1990The H3-histamine receptor provides feedback inhibition of histamine synthesis and release as well as inhibition of other neurotransmitter release. We have characterized this receptor by radioligand binding studies with the H3 agonist N alpha-[3H]methylhistamine ([3H]NAMHA).
R E, West +5 more
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Phencyclidine blocks histamine H3-receptors in rat brain
European Journal of Pharmacology, 1988Phencyclidine (PCP) was examined for its ability to modulate histamine release from rat brain slices labeled with L-[3H]histidine. PCP failed to mimic but completely reversed the autoinhibitory effect of histamine at H3-receptors with an apparent Ki value of 13 +/- 3 microM.
Jean-Charles Schwartz +2 more
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2003
Some G-protein-coupled receptors display constitutive activity, that is spontaneous activity in the absence of agonist: a proportion of the receptor population adopts a conformation that can bind and activate G proteins. Whereas this was mainly shown to occur with recombinant or pathologically mutated receptors, the physiological relevance of the ...
Schwartz, J. C. +9 more
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Some G-protein-coupled receptors display constitutive activity, that is spontaneous activity in the absence of agonist: a proportion of the receptor population adopts a conformation that can bind and activate G proteins. Whereas this was mainly shown to occur with recombinant or pathologically mutated receptors, the physiological relevance of the ...
Schwartz, J. C. +9 more
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Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors
Neuroscience, 1987The regulation of histamine synthesis was studied on rat brain slices or synaptosomes labeled with L-[3H]histidine. Depolarization by increased extracellular K+ concentration enhanced by about twofold the [3H]histamine formation in slices of cerebral cortex.
J.-C. Schwartz +2 more
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1998
Publisher Summary Histamine is released in the brain from neurons projecting in a diffuse manner to widely divergent cerebral areas and arising from the tuberomammillary nucleus of the posterior hypothalamus. It affects target cells via the activation of three receptor subtypes that are termed H 1 , H 2 , and H 3 .
S. Morisset +3 more
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Publisher Summary Histamine is released in the brain from neurons projecting in a diffuse manner to widely divergent cerebral areas and arising from the tuberomammillary nucleus of the posterior hypothalamus. It affects target cells via the activation of three receptor subtypes that are termed H 1 , H 2 , and H 3 .
S. Morisset +3 more
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Fluorinated non-imidazole histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2009Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (
Holger Stark +8 more
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Molecular analysis of the histamine H3-receptor
2010The histamine H3 receptor (H3R) is a biogenic amine receptor that belongs to family I of G protein-coupled receptors (GPCRs). During the past two decades, the H3R has gained much interest in academia and industry. The H3Rs is predominantly localized in the brain and regulates the release of histamine as well as other neurotransmitters into the synaptic
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