Search Results - "Hancock, Arthur A."
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4-(2-[2-(2(R)-Methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and Related 2-Aminoethylbenzofuran H3 Receptor Antagonists Potently Enhance Cognition and Attention
Published in Journal of medicinal chemistry (13-01-2005)“…H3 receptor antagonists based on a 2-aminoethylbenzofuran skeleton have been discovered, which are potent in vitro at human and rat H3 receptors, with K i…”
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Perspectives on cognitive domains, H3 receptor ligands and neurological disease
Published in Expert opinion on investigational drugs (01-10-2004)“…Histamine H(3) receptor agonists and antagonists have been evaluated in numerous in vitro and in vivo animal models to better understand how H(3) receptors…”
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A new class of potent non-imidazole H3 antagonists: 2-aminoethylbenzofurans
Published in Bioorganic & medicinal chemistry letters (01-02-2004)Get full text
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Two novel and selective nonimidazole H3 receptor antagonists A-304121 and A-317920: II. In vivo behavioral and neurophysiological characterization
Published in The Journal of pharmacology and experimental therapeutics (01-06-2003)“…Pharmacological blockade of central histamine H3 receptors (H3Rs) enhances cognition in rodents and offers promise for the clinical treatment of neurological…”
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Effects of histamine H3 receptor antagonists in two models of spatial learning
Published in Behavioural brain research (30-04-2005)“…Despite the well-described attention and short-term memory enhancing effects of H3 receptor antagonists, and evidence to suggest a close relationship between…”
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An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity
Published in The Journal of pharmacology and experimental therapeutics (01-12-2007)“…In this article, we pharmacologically characterized two naturally occurring human histamine H3 receptor (hH3R) isoforms, hH3R(445) and hH3R(365). These…”
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Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects
Published in The Journal of pharmacology and experimental therapeutics (01-06-2003)“…Histamine H3 receptor (H3R) antagonists enhance neurotransmitter release and are being developed for the treatment of a variety of neurological and cognitive…”
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Structure–activity relationships of arylbenzofuran H3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (16-05-2005)“…An SAR study of histamine H3 receptor antagonists based on substituted (R)-2-methyl-1-[2-(5-phenyl-benzofuran-2-yl)-ethyl]-pyrrolidines is presented. An SAR…”
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Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist
Published in Biochemical pharmacology (01-09-2004)“…Histamine H3 receptors regulate the release of a variety of central neurotransmitters involved in cognitive processes. A-349821…”
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Enhancement of prepulse inhibition of startle in mice by the H3 receptor antagonists thioperamide and ciproxifan
Published in Behavioural brain research (12-08-2004)“…Histamine H3 receptor antagonists/inverse agonists have been proposed as potential therapeutic agents for the treatment of a number of neurological disorders…”
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G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations
Published in The Journal of pharmacology and experimental therapeutics (01-07-2005)“…Previously reported pharmacological studies using the imidazole-containing histamine H3 receptor ligands GT-2331 (Cipralisant) and proxyfan resulted in a range…”
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Design of a New Histamine H3 Receptor Antagonist Chemotype: (3aR,6aR)-5-Alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, Synthesis, and Structure−Activity Relationships
Published in Journal of medicinal chemistry (13-08-2009)“…A new histamine H3 receptor (H3R) antagonist chemotype 1 was designed by combining key pharmacophoric elements from two different precursor structural series…”
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In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists : Trends across multiple chemical series
Published in Bioorganic & medicinal chemistry letters (2008)“…Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were…”
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An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute Configuration
Published in Journal of organic chemistry (09-01-2004)“…GT-2331 is a potent histamine H3 antagonist which has entered clinical trials. Efficient multigram syntheses of this compound and its enantiomer are described…”
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Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: Novel and selective histamine H3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (07-04-2003)“…Novel 4'-[(NR1R2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H(3)receptors. Most…”
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Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model
Published in Pharmacology, biochemistry and behavior (01-06-2002)“…The selective H(3) receptor agonist (R)-alpha-methylhistamine [(R)-alpha-MeHA] stimulates drinking in the adult rat. In the present study, we investigated the…”
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Use of a fluorescent imaging plate reader--based calcium assay to assess pharmacological differences between the human and rat vanilloid receptor
Published in Journal of biomolecular screening (01-10-2002)“…The cloned vanilloid receptor 1 (VR1) is a ligand-gated calcium channel that is believed to be the capsaicin-activated vanilloid receptor found in native…”
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Pharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist
Published in The Journal of pharmacology and experimental therapeutics (01-10-2012)“…Blockade of the histamine H(3) receptor (H(3)R) enhances central neurotransmitter release, making it an attractive target for the treatment of cognitive…”
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Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist
Published in The Journal of pharmacology and experimental therapeutics (01-04-2005)“…Acute pharmacological blockade of central histamine H3 receptors (H3Rs) enhances arousal/attention in rodents. However, there is little information available…”
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