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246 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27866818 84 The discovery of quinoline based single-ligand human HEBI GlaxoSmithKline Medicines Research Centre
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27692832 7 Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.EBI Bioprojet-Biotech
27584694 103 Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.EBI Icahn School of Medicine at Mount Sinai
27502700 36 Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.EBI Novartis Institutes of Biomedical Research (NIBR)
27007611 115 Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI University of Regensburg
26741166 105 Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.EBI AstraZeneca
26390077 42 Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI University of Minnesota
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26731168 39 Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.EBI Suven Life Sciences Ltd
26718844 55 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.EBI Friedrich-Alexander-Universit£t Erlangen-N£rnberg
26690914 22 Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents.EBI Jagiellonian University Medical College
25993395 19 Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI Janssen Research& Development, LLC
25893048 25 Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.EBI Janssen Pharmaceutical Company
25941545 21 Biphenyl-ethyl-pyrrolidine derivatives as histamine h3 receptor modulators for the treatment of cognitive disorders.EBI Temple University School of Pharmacy
25827402 54 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.EBI Teva Global R&D.
25703249 132 Novel 4-substituted-N,N-dimethyltetrahydronaphthalen-2-amines: synthesis, affinity, and in silico docking studies at serotonin 5-HT2-type and histamine H1 G protein-coupled receptors.EBI University of Florida
25047936 183 Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.EBI Universit£t Regensburg
25218907 18 Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.EBI University of Catania
24996140 26 Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.EBI Jagiellonian University Medical College
24745967 19 Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.EBI Johann Wolfgang Goethe University
24495018 77 Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.EBI Janssen Research& Development, LLC
24650714 21 Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.EBI United Arab Emirates University
24050887 49 Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.EBI Merck Research Laboratories
23218604 30 Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold.EBI KU Leuven
16610798 5 A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.EBI Vrije Universiteit Amsterdam
22222138 40 Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain.EBI Universit£ degli Studi di Parma
22003888 41 Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.EBI VU University Amsterdam
21348462 64 Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.EBI VU University Amsterdam
20409707 66 Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.EBI University of Regensburg
20171098 20 Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.EBI Abbott Laboratories
19791743 41 Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.EBI University of Regensburg
19524331 33 Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.EBI Johnson& Johnson Pharmaceutical Research& Development
19414267 49 Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.EBI VU University Amsterdam
18990469 23 Non-imidazole histamine H3 ligands, part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.EBI Medical University
19317445 53 N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.EBI University of Regensburg
18976927 83 Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.EBI Universit£ degli Studi di Parma
15771465 56 4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.EBI Johnson& Johnson Pharmaceutical Research and Development
15115383 1 Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.EBI Vrije Universiteit Amsterdam
14640554 31 N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.EBI Freie Universit£t Berlin
12930154 6 A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.EBI Johnson& Johnson Pharmaceutical Research& Development
10794692 15 Characterization of the binding site of the histamine H(3) receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide.EBI Vrije Universiteit
10737740 57 Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.EBI Freie Universit£t Berlin
9258364 10 H3-receptor antagonists: synthesis and structure-activity relationships of para- and meta-substituted 4(5)-phenyl-2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazoles.EBI Universit£ degli Studi di Parma
7830269 9 Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole.EBI Vrije Universiteit Amsterdam
7783156 35 New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent.EBI Vrije Universiteit Amsterdam
12657274 2 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott Laboratories
9873585 30 N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.EBI Freie Universit£t Berlin
23099096 88 Novel azulene derivatives for the treatment of erectile dysfunction.EBI Friedrich Alexander University
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI The University of Sydney
22483590 5 Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.EBI ETH Zurich (Swiss Federal Institute of Technology)
21928839 51 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).EBI Pfizer Inc.
22216892 66 The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.EBI University of Regensburg
22985961 99 Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
22578490 35 Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22450133 64 Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists.EBI Cephalon, Inc.
22617490 23 Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.EBI Cephalon, Inc.
22607684 50 7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.EBI The University of Sydney
22464130 27 Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.EBI Merck Research Laboratories
22313242 146 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI Pfizer Inc.
22313227 78 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.EBI National Institute of Mental Health
22444026 103 Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies.EBI Universidad de Navarra
22365751 45 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.EBI Cephalon, Inc.
21906941 94 Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists.EBI Cephalon, Inc.
21782432 62 Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.EBI Cephalon, Inc.
21824776 31 Amine-constrained pyridazinone histamine H3 receptor antagonists.EBI Cephalon Inc.
21634396 55 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.EBI Cephalon, Inc.
21207959 69 Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI National Institute of Mental Health
20684563 176 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI H. Lundbeck A/S
20541426 46 Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI Meiji Seika Kaisha, Ltd
20561786 77 Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C.
20299215 49 Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.EBI Argenta Discovery Ltd.
19963380 38 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI Hunter College and the Graduate Center of the City University of New York
19456097 89 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.EBI F. Hoffmann-La Roche Ltd.
19091563 79 Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.EBI Johann Wolfgang Goethe Universit£t
19329325 20 Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.EBI Jagiellonian University Medical College
18950149 75 Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI University of Regensburg
18606542 7 Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.EBI F. Hoffmann-La Roche Ltd.
18468904 48 High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI Purdue University
18249544 12 Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.EBI Johnson& Johnson Pharmaceutical Research and Development
18077160 126 In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI Abbott Laboratories
18060777 158 Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C.
18052318 30 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.EBI GlaxoSmithKline Medicines REsearch Centre
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15634000 57 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.EBI Abbott Laboratories
15139761 33 1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.EBI Novo Nordisk A/S
12672253 60 Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.EBI Freie Universit£t Berlin
12954048 36 The first potent and selective non-imidazole human histamine H4 receptor antagonists.EBI Johnson& Johnson Pharmaceutical Research and Development
12190321 55 Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.EBI Freie Universit£t Berlin
11356102 16 Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.EBI De Novo Pharmaceuticals
22326166 40 Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.EBI Merck Research Laboratories
22297111 32 Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.EBI Cephalon, Inc.
22290075 60 4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity.EBI Cephalon, Inc.
22197136 29 Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.EBI Cephalon, Inc.
22189138 62 Synthesis of novel histamine H4 receptor antagonists.EBI Pfizer Inc.
22172695 28 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).EBI Arena Pharmaceuticals
22153663 59 Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.EBI Griffin Discoveries BV
22153342 60 Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22142542 73 4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists.EBI Cephalon, Inc.
22019465 28 Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.EBI Zhejiang University
22014551 33 Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI Cephalon, Inc.
22007643 25 Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.EBI VU University Amsterdam
21955944 39 Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).EBI Pfizer Inc.
21944855 30 Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.EBI Cephalon, Inc.
21937153 46 Recent progress in synthesis and bioactivity studies of indolizines.EBI University of Botswana
21843941 40 Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists.EBI Pfizer Inc.
21802950 466 Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity.EBI Bioprojet-Biotech
21783360 52 Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.EBI Bioprojet-Biotech
19577344 43 Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.EBI Johnson& Johnson Pharmaceutical Research and Development
21498080 45 N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.EBI Jagiellonian University Medical College
21186123 36 Discovery of a series of potent arylthiadiazole H(3) antagonists.EBI Merck Research Laboratories
20945906 33 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.EBI Abbott Laboratories
20932767 66 Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.EBI Universidad de Navarra
20843691 26 Indole- and benzothiophene-based histamine H3 antagonists.EBI Johnson& Johnson Pharmaceutical Research& Development
20833043 28 Investigation of 4-piperidinols as novel H3 antagonists.EBI Athersys Inc.
20812727 157 Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI National Institute of Mental Health
20801030 106 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.EBI F Hoffmann-La Roche Ltd
20728354 16 Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.EBI Johann Wolfgang Goethe University
20727744 10 Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.EBI Johann Wolfgang Goethe University
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20690643 68 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI Meiji Seika Kaisha, Ltd.
20685118 97 The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.EBI Merck Research Laboratories
20667729 86 Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI Evotec (UK) Ltd
20457525 225 In vitro studies on a class of quinoline containing histamine H3 antagonists.EBI Abbott Laboratories
20452213 65 Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI Johnson& Johnson Pharmaceutical Research& Development
20397706 7 Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy.EBI Hokkaido University
20384344 42 Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI Meiji Seika Kaisha, Ltd.
20382018 81 Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C.
20188550 41 Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.EBI Merck Research Laboratories
19846299 52 Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.EBI Jagiellonian University Medical College
20045649 5 Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.EBI Hokkaido University
20042333 21 Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.EBI Wyeth Research
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19773164 53 Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.EBI Schering-Plough Research Institute
19524437 31 Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.EBI Hoffmann-La Roche Ltd
19722526 30 Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.EBI Arena Pharmaceuticals
19520574 49 Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI Tsukuba Research Institute
19553110 16 Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.EBI Tsukuba Research Institute
19588934 71 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.EBI Abbott Laboratories
19443215 74 A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.EBI Vanderbilt University
18922693 37 2-Aryloxymethylmorpholine histamine H(3) antagonists.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C.
 21 Unsymmetrically substituted guanidines as potent histamine H3-receptor antagonistsEBI TBA
 2 Two novel, potent and selective histamine H3 receptor agonistsEBI TBA
19329329 183 Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
19286376 17 Fluorinated non-imidazole histamine H3 receptor antagonists.EBI Johann Wolfgang Goethe-Universität
19119007 34 Novel imidazole-based histamine H3 antagonists.EBI Johnson & Johnson Pharmaceutical Research & Development
18952421 60 Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18841880 82 Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18800848 8 Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.EBI Vanderbilt University
18783208 11 Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI National Institute of Mental Health
18774720 14 Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.EBI Jagiellonian University Medical College
18768318 37 Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18754613 23 Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.EBI National Institute of Mental Health
18752952 31 Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.EBI The Schering Plough Research Institute
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18554904 26 Novel H3 receptor antagonists with improved pharmacokinetic profiles.EBI Arena Pharmaceuticals
18353639 27 Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.EBI Kyowa Hakko Kogyo Co. Ltd
17918921 35 Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.EBI Abbott Laboratories
17616397 107 Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development LLC
17583504 51 Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17571866 49 Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI National Institute of Mental Health
17524641 69 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI GlaxoSmithKline
17498953 17 A new class of histamine H3 receptor antagonists derived from ligand based design.EBI F. Hoffmann-La Roche Ltd
17412583 81 Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.EBI Johnson & Johnson Pharmaceutical Research & Development
17317177 69 Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development L.L.C.
17307358 81 Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17169555 46 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.EBI Abbott Laboratories
17127059 96 Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development L.L.C.
17107798 90 Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.EBI Johnson & Johnson Pharmaceutical Research and Development LLC
16942032 64 Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI Hokkaido University
16908150 59 Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.EBI Novo Nordisk A/S
16677814 67 Synthesis and SAR of novel histamine H3 receptor antagonists.EBI Lilly Research Laboratories
16616493 14 Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor.EBI Novo Nordisk A/S
16458504 37 Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI Columbia University College of Physicians and Surgeons
16434192 6 Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.EBI Johann Wolfgang Goethe-Universität
16392798 46 Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI Columbia University College of Physicians and Surgeons
16366610 41 Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
16300945 21 Aplysamine-1 and related analogs as histamine H3 receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
16297617 87 Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.EBI The Schering Plough Research Institute
16246552 57 Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.EBI The Schering Plough Research Institute
16190774 60 Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.EBI Abbott Laboratories
15634025 29 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI Novo Nordisk A/S
15115409 72 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.EBI Freie Universität Berlin
14741270 76 A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.EBI Abbott Laboratories
14741266 203 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.EBI Abbott Laboratories
12798320 12 A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.EBI Abbott Laboratories
12781173 28 Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.EBI The Schering-Plough Research Institute
12729661 20 Non-imidazole heterocyclic histamine H3 receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development L. L. C.
12723960 58 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.EBI Hokkaido University
12392739 43 Novel human histamine H(3) receptor antagonists.EBI Johnson and Johnson Pharmaceutical Research and Development
12182878 13 The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.EBI The Schering Plough Research Institute
11958998 22 Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.EBI The Schering Plough Research Institute
11855993 91 Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.EBI Freie Universität Berlin
11294398 26 Different antagonist binding properties of human and rat histamine H3 receptors.EBI Freie Universität Berlin
10882362 2 Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.EBI The James Black Foundation
9873525 13 4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor.EBI Schering-Plough Research Institute
9873505 48 Novel H3 receptor antagonists. Sulfonamide homologs of histamine.EBI Schering-Plough Research Institute
9871662 15 Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.EBI Schering-Plough Research Institute
7752184 12 A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.EBI Schering-Plough Research Institute
17221184 55 Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.BDB Columbia University
16915381 31 WAY-100635 is a potent dopamine D4 receptor agonist.BDB Purdue University
16675639 28 Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.BDB Wyeth Research
15608078 35 Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.BDB Abbott Laboratories
15466448 7 Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.BDB Johnson & Johnson Pharmaceutical Research and Development, LLC
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
15033391 33 Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.BDB Abbott Laboratories
12784105 53 Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.BDB Case Western Reserve University
12721338 61 N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.BDB Pudue Pharma Discovery Research
12649305 4 Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).BDB Schering-Plough Research Institute
12606603 59 Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.BDB Abbott Laboratories
12527336 21 Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.BDB Aventis Pharma
11714875 18 Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.BDB Vrije Universiteit
11179436 9 Cloning, expression, and pharmacological characterization of a novel human histamine receptor.BDB SmithKline Beecham Pharmaceuticals
11179434 31 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.BDB The R. W. Johnson Pharmaceutical Research Institute
10869375 23 Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.BDB R. W. Johnson Pharmaceutical Research Institute
10347254 11 Cloning and functional expression of the human histamine H3 receptor.BDB R.W. Johnson Pharmaceutical Research Institute
10215699 19 Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.BDB Gliatech Inc.
9454810 72 SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB Sanofi Recherche
8891613 25 Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320.BDB Glaxo Research & Development Ltd.
8564266 77 Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.BDB Vrije Universiteit
8012715 38 GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.BDB Glaxo Group Research Ltd.
7965746 33 [125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.BDB U. 109
7473144 1 Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies.BDB Gliatech, Inc.
2848779 9 Highly potent and selective ligands for a new class H3 of histamine receptor.BDB Unité 109
2213013 14 Biexponential kinetics of (R)-alpha-[3H]methylhistamine binding to the rat brain H3 histamine receptor.BDB Schering-Plough Research
1321744 14 Multiple histamine receptors: properties and functional characteristics.BDB Queen's Medical Centre
18683917 57 The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.BDB Abbott Laboratories
18811133 12 Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.BDB Abbott Laboratories
18983139 12 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia.BDB Abbott Laboratories
15947036 80 Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.BDB Vrije Universiteit Amsterdam
14722321 9 A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.BDB Johnson & Johnson Pharmaceutical
18433114 28 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.BDB VU University Amsterdam