Histamine is an intriguing compound; the same is true for the several classes of anti-histaminergic compounds. The classical anti-histamines, now known as H -antagonists have 1 been the result of intensive research in the 1950s and 1960s. The new, so-called non-sedating H1-antagonists, which became available in the 1980s, could be d'eveloped mainly due to insights into structural features causing the sedating effects of the older compounds. In the 1970s the H2-receptors became important targets for developing new anti-ulcer agents. The H2-antagonist story is a stimulating example of modern research on pharmacology and medicinal chemistry. Unknown and new properties of histamine and histaminergic systems came to the attention of the pharmacologists and medicinal chemists in the 1980s. The role of histamine as a neurotransmitter, the existence of a presynaptic receptor (H ) controlling the release of histamine 3 and other neurotransmitters, and the particular character of this receptor became important as the possibilities to design new therapeutic agents were realized. Recently, other roles of the histaminergic systems have been suggested. Is there a distinct histamine receptor involved in immunological features of histamine? Is histamine involved in the prolactin axis? Are histamine receptors intracellularly present in certain cells and what is their possible role? For these reasons it was the right time to discuss "New Perspectives in Histamine Research" during a scientific meeting. Therefore a symposium was organized as a satellite of the XIth International Congress of Pharmacology of IUPHAR in Amsterdam in 1990.
Table of Contents
Histaminergic neuron system: Morphological features and possible functions.- Neuroendocrine functions of histamine.- The histamine H3-receptor: Pharmacology, roles and clinical implications studied with agonists.- Characterisation of the binding of the histamine H3 receptor agonist [3H](R)-alpha methyl histamine to homogenates of rat and guinea-pig cortex.- The significance of brain histamine and its receptors in opoid stimulation of the pituitary-adrenocortical activity.- Importance of histamine for seizure susceptibility.- Hypothalamic neuronal histamine modulates energy balance in rats.- Role of histamine in pathophysiology of stress in rats.- Histamine receptors in the lung.- Reversible and irreversible labelling of H1- and H2-receptors using novel [125I]probes.- Histamine receptors and interactions between second messenger transduction systems.- Histamine H1-receptors on astrocytes in primary cultures: A possible target for histaminergic neurons.- Pharmacology of non-sedating H1 antihistamines.- Controlled clinical trials and cross-sectional studies with histamine measurements and histamine receptor antagonists: solving the problem of preoperative H1- + H2-prophylaxis by asking new questions?.- Structure-activity relationships of histamine H2-agonists, a new class of positive inotropic drugs.- Therapeutic value of H2-receptor stimulation in congestive heart failure. Hemodynamic effects of BU-E-76, BU-E-75 and arpromidine (BU-E-50) in comparison to impromidine.- Inhibition by cations of antagonist binding to histamine H1-receptors.- Novel chiral H3-receptor agonists.- The effects of (R)-methyl histamine on the isolated guinea pig aorta.- Multiple signaling pathways of histamine H2 receptors.- Histamine H2-receptor in atrium: Signal transduction and response.- 4- or 5-(?-aminoalkyl)thiazoles and derivatives; new selective H2-receptor agonists.- Theoretical analysis of the activity of dimaprit derivatives on the H2-receptor.- The antiproliferative potency of histamine antagonists correlates with inhibition of binding of [3H)-histamine to novel intracellular receptors (HIC) in microsomal and nuclear fractions of rat liver.- Histamine metabolites and Pros-methylimidazoleacetic acid in human cerebrospinal fluid.- Histamine and its congener derivatives as immune modulators.- Labeling of histamine H1-receptors in vivo: A compartiment model analysis and positron emission tomographic imaging.- Characteristics of histamine-induced inositol phospholipid hydrolysis in Hela cells.- Is protein kinase c involved in histamine H1-receptor desensitization?.- Investigation of the antihistaminic action of dimethindene maleate (FenistilR) and its optical isomers.- The inhibiting effect of cetirizine 2HC1 on eosinophil migration and its link to H1 blockade.- Calcium signal and histamine secretion induced by aggregation of immunoglobulin E receptors in rat basophilic leukemia(RBL-2H3) cells.- Rat mast cells inhibit platelet aggregation by releasing a nitric oxide-like factor: Influence on histamine release.- Pentagastrin-stimulated histamine release and acid secretion from the totally isolated vascularly perfused rat stomach.