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Journals and Conferences
New drugs selective for histamine H3-receptors can be used to establish that these receptors are involved in the feedback control of histamine synthesis and release, and to demonstrate their distribution in the brain and peripheral tissues. These drugs provide new tools for affecting physiological and possibly pathological conditions in which histamine is… (More)
In contrast to cerebral histamine H1 and H2-receptors, histamine H3-receptors are presynaptically located on histamine-synthesizing nerve terminals (autoreceptors) and control the synthesis and release of the amine in cerebral neurons. Two imidazole derivatives were designed to interact at H3-receptors: (R) alpha-methylhistamine (alpha-MeHA), a chiral… (More)
Thirteen 5,11-dimethyl-6H-pyrido[3,2-b]carbazoles, structurally related to the antitumour drug ellipticine, were tested for their cytotoxicity against the L1210 murine leukaemia cell line and their antitumour activity against both leukaemias and solid tumours. Most of them showed an interesting antitumour activity against L1210 leukaemia,… (More)
The third histamine receptor was first identified on brain neurons and seems also to be present in other cells such as the lung mast cells. Hence the novel and potent H3 receptor agonist (R)-alpha-methylhistamine might find therapeutic applications in allergic diseases.
A series of piperazinopyrrolo[1,2-a]thieno[3,2-e]- and -[2,3-e]pyrazine derivatives were prepared and evaluated in order to determine the necessary requirements for high affinity on the 5-HT3 receptors and high selectivity versus other 5-HT receptor subtypes. Various substitutions on the piperazine and the thiophene ring of the pyrrolothienopyrazine… (More)
The first medical cure of Acanthamoeba keratitis was obtained by use of propamidine isethionate. Since then, it has been the basic drug recommended for use in treatment. Because some Acanthamoeba strains have been reported to be resistant to propamidine and propamidine was found to be only weakly cysticidal, superior homologs such as butamidine,… (More)
Cetiedil is a potent blocker of acetylcholine and choline fluxes. Several analogs of this compound have been synthesized and their effect on acetylcholine (ACh) and choline fluxes in synaptosomes and on ACh uptake in synaptic vesicles have been studied. The effects of these analogs were compared to those of other drugs acting on cholinergic functions. All… (More)
The third histamine receptor was first indentified on brain neurons and seems to be present in other cells such as lung mast cells. Hence the novel and potent H3-receptor agonist (R) alpha-methylhistamine might find therapeutic applications in allergic diseases.
The DNA sequences targeted by a complete homologous series of aromatic diamidines have been determined at single-nucleotide resolution via protection from cutting by the endonucleases DNase I, DNase II and micrococcal nuclease. Propamidine, pentamidine and to a lesser extent hexamidine bind selectively to nucleotide sequences composed of at least four… (More)
The ability of two S,S'-(alkane-1,omega-diyl) bisisothiouronium dibromides, three N,N'-(alkane-1, omega-diyl) bis guanidinium dinitrates and N,N'-bis (3-guanidinopropyl)piperazine dinitrate to inhibit constitutive (i.e. endothelial and neuronal forms) and inducible forms of nitric oxide synthases has been evaluated in vivo. These compounds, synthesized by… (More)