110 articles for thisTarget
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Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.
Abbott Laboratories
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.
Teva Global R & D.
Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.
University Of Catania
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.
Johann Wolfgang Goethe University
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.
Teva Pharmaceutical Global R & D
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Glaxosmithkline
The discovery of the benzazepine class of histamine H3 receptor antagonists.
Glaxosmithkline
Identification and profiling of 3,5-dimethyl-isoxazole-4-carboxylic acid [2-methyl-4-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)phenyl] amide as histamine H(3) receptor antagonist for the treatment of depression.
Sanofi Us
Synthesis, characterization, and biological assessment of the four stereoisomers of the H(3) receptor antagonist 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl[1,3']bipyrrolidinyl-1'-yl)phenyl]benzamide.
Sanofi Us
Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II).
Sanofi Us
Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part I).
Sanofi Us
Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain.
Universit£
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Abbott Laboratories
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.
Universit£
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
Abbott Laboratories
Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity
TBA
Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
Eth Zurich (Swiss Federal Institute Of Technology)
Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Pfizer
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.
Cephalon
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists.
Cephalon
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.
Cephalon
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.
Pfizer
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute Of Mental Health
Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.
Cephalon
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists.
Cephalon
Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.
Cephalon
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Cephalon
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Johnson & Johnson Pharmaceutical Research & Development
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
F. Hoffmann-La Roche
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
Jagiellonian University Medical College
A new family of H3 receptor antagonists based on the natural product Conessine.
Arena Pharmaceuticals
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Abbott Laboratories
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.
Abbott Laboratories
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.
Freie Universit£T Berlin
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
De Novo Pharmaceuticals
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.
Freie Universit£T Berlin
Diastereoselective synthesis of trans-2-(1-triphenylmethyl-1H-imidazol-4-yl)cyclopropanecarboxylic acids: key intermediates for the preparation of potent and chiral histamine H3 receptor agents
TBA
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.
Cephalon
4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity.
Cephalon
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.
Cephalon
Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).
Arena Pharmaceuticals
Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.
Griffin Discoveries
Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.
Cephalon
4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists.
Cephalon
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.
Cephalon
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.
Cephalon
Recent progress in synthesis and bioactivity studies of indolizines.
University Of Botswana
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research And Development
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Abbott Laboratories
Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.
F. Hoffmann-La Roche
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.
Evotec (Uk)
In vitro studies on a class of quinoline containing histamine H3 antagonists.
Abbott Laboratories
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Jagiellonian University Medical College
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Wyeth Research
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.
Arena Pharmaceuticals
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.
Tsukuba Research Institute
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
Tsukuba Research Institute
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.
Abbott Laboratories
2-Aryloxymethylmorpholine histamine H(3) antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Imetit and N-methyl derivatives. The transition from potent agonist to antagonist at histamine H3 receptors.1
TBA
Novel imidazole-based histamine H3 antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.
Vanderbilt University
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Arena Pharmaceuticals
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
Kyowa Hakko Kogyo
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
Abbott Laboratories
A new class of histamine H3 receptor antagonists derived from ligand based design.
F. Hoffmann-La Roche
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
Abbott Laboratories
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
Abbott Laboratories
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
University College London
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
Freie UniversitäT Berlin
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Abbott Laboratories
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.
Abbott Laboratories
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.
Hokkaido University
Novel human histamine H(3) receptor antagonists.
Johnson And Johnson Pharmaceutical Research And Development
Different antagonist binding properties of human and rat histamine H3 receptors.
Freie UniversitäT Berlin
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Freie UniversitäT Berlin
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Freie UniversitäT Berlin
Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.
Freie UniversitäT Berlin
Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists.
Gliatech
Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.
Freie UniversitäT Berlin
General construction pattern of histamine H3-receptor antagonists: change of a paradigm.
Freie UniversitäT Berlin
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Gliatech
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
Freie UniversitäT Berlin
A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists.
University College London
Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.
Freie UniversitäT Berlin
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
Freie UniversitäT Berlin
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Design of potent non-thiourea H3-receptor histamine antagonists.
University College London
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
Vrije Universiteit
Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
UniversitÉ