359 articles for thisTarget
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Article Title
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Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.
Abbott Laboratories
4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists.
The James Black Foundation
From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.
The James Black Foundation
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.
Bioprojet-Biotech
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.
Icahn School of Medicine At Mount Sinai
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.
Novartis Institutes of Biomedical Research (Nibr)
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.
University of Regensburg
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.
Astrazeneca
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
Suven Life Sciences
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents.
Jagiellonian University Medical College
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
Janssen Research and Development
Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.
Janssen Pharmaceutical Companies of Johnson & Johnson
Biphenyl-ethyl-pyrrolidine derivatives as histamine h3 receptor modulators for the treatment of cognitive disorders.
Temple University
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.
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.
University of Florida
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.
Universit£T Regensburg
Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.
University of Catania
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.
Jagiellonian University Medical College
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.
Johann Wolfgang Goethe University
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.
Janssen Research and Development
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
United Arab Emirates 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 and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.
Merck Research Laboratories
Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity.
Merck Research Laboratories
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
Novel and highly potent histamine H3 receptor ligands. Part 3: an alcohol function to improve the pharmacokinetic profile.
Bioprojet-Biotech
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.
Goethe University
Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold.
Ku Leuven
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.
Vrije Universiteit Amsterdam
Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain.
University of Parma
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.
Vu University Amsterdam
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.
Vu University Amsterdam
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.
University of Regensburg
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Abbott Laboratories
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.
University of Regensburg
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.
Johnson & Johnson Pharmaceutical Research & Development
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Vu University Amsterdam
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.
University of Regensburg
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.
University of Parma
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.
Johnson & Johnson Pharmaceutical Research and Development
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
Novel azulene derivatives for the treatment of erectile dysfunction.
Friedrich-Alexander University
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).
The University of Sydney
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
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.
University of Regensburg
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
Glaxosmithkline
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.
TBA
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
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.
The University of Sydney
Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.
Merck Research Laboratories
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
Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies.
Universidad De Navarra
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
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
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
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.
H. Lundbeck
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.
Meiji Seika Kaisha
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Johnson & Johnson Pharmaceutical Research & Development
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Argenta Discovery
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
F. Hoffmann-La Roche
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.
Johann Wolfgang Goethe Universit£T
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
Jagiellonian University Medical College
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
University of Regensburg
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.
F. Hoffmann-La Roche
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Purdue University
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
Johnson & Johnson Pharmaceutical Research and Development
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
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.
Glaxosmithkline
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
University of Urbino
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
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
Novo Nordisk
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
Freie Universit£T Berlin
The first potent and selective non-imidazole human histamine H4 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
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
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
Merck Research Laboratories
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
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.
Zhejiang University
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.
Cephalon
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.
Vu University Amsterdam
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).
Pfizer
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
Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity.
Bioprojet-Biotech
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.
Bioprojet-Biotech
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
Jagiellonian University Medical College
Discovery of a series of potent arylthiadiazole H(3) antagonists.
Merck Research Laboratories
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
Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.
Universidad De Navarra
Indole- and benzothiophene-based histamine H3 antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
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
Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.
Johann Wolfgang Goethe University
Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
Johann Wolfgang Goethe University
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.
Meiji Seika Kaisha
The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
Merck Research Laboratories
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
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.
Johnson & Johnson Pharmaceutical Research & Development
Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy.
Hokkaido University
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.
Meiji Seika Kaisha
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
Merck Research Laboratories
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Jagiellonian University Medical College
Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.
Hokkaido University
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Wyeth Research
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.
Schering-Plough Research Institute
Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.
Hoffmann-La Roche
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
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.
Vanderbilt University
2-Aryloxymethylmorpholine histamine H(3) antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Verongamine, a Novel Bromotyrosine-Derived Histamine H3-Antagonist from the Marine Sponge Verongula gigantea
TBA
Imetit and N-methyl derivatives. The transition from potent agonist to antagonist at histamine H3 receptors.1
TBA
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
Fluorinated non-imidazole histamine H3 receptor antagonists.
Johann Wolfgang Goethe-UniversitäT
Novel imidazole-based histamine H3 antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Tsukuba Research Institute
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 and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
National Institute of Mental Health
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Jagiellonian University Medical College
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.
Tsukuba Research Institute
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.
National Institute of Mental Health
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.
The Schering Plough Research Institute
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
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
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.
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
A new class of histamine H3 receptor antagonists derived from ligand based design.
F. Hoffmann-La Roche
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT
University of Texas Medical Branch (UTMB)
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.
University of Michigan
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
Abbott Laboratories
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.
Johnson & Johnson Pharmaceutical Research and Development
Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H
Universidade Federal De Sao Paulo
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.
Hokkaido University
Rational Multitargeted Drug Design Strategy from the Perspective of a Medicinal Chemist.
Shandong University
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
Novo Nordisk
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H
University of Nottingham Biodiscovery Institute
Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor.
Novo Nordisk
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.
Columbia University College of Physicians and Surgeons
Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.
Johann Wolfgang Goethe-UniversitäT
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.
Columbia University College of Physicians and Surgeons
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
The Schering Plough Research Institute
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
The Schering Plough Research Institute
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
Abbott Laboratories
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Novo Nordisk
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
University of Regensburg
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
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
Huazhong University of Science and Technology
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H
University of Regensburg
Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease.
Zhejiang University
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
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
The Schering Plough Research Institute
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.
Sungkyunkwan University
Non-imidazole heterocyclic histamine H3 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
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
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H
Zhejiang University
Structural modifications in the distal, regulatory region of histamine H
Jagiellonian University Medical College
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Soochow University
Novel human histamine H(3) receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.
The Schering Plough Research Institute
Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.
Zhejiang University
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
Jagiellonian University Medical College
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H
Universidade Federal De S£O Paulo
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
The Schering Plough Research Institute
Novel pyrrolidinone derivative lacks claimed histamine H
Heinrich Heine University D£Sseldorf
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Freie UniversitäT Berlin
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Astrazeneca
In silico and in vitro studies on interaction of novel non-imidazole histamine H
Jagiellonian University Medical College
Different antagonist binding properties of human and rat histamine H3 receptors.
Freie UniversitäT Berlin
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H
University of Regensburg
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Freie UniversitäT Berlin
Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands.
Gedeon Richter
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Freie UniversitäT Berlin
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
Peking Union Medical College
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H
Jagiellonian University Medical College
Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.
The James Black Foundation
Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands.
Jagiellonian University Medical College
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.
Freie UniversitäT Berlin
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
Academy of Scientific and Innovative Research (Acsir)
Optimization and preclinical evaluation of novel histamine H
Jagiellonian University Medical College
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
Search for new multi-target compounds against Alzheimer's disease among histamine H
Jagiellonian University Medical College
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H
Suven Life Sciences
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor.
Schering-Plough Research Institute
Novel H3 receptor antagonists. Sulfonamide homologs of histamine.
Schering-Plough Research Institute
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
Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.
Schering-Plough Research Institute
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H
Vrije Universiteit Amsterdam
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
Freie UniversitäT Berlin
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
Csir-Central Drug Research Institute
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H
Heinrich Heine University D£Sseldorf
Synthesis and evaluation of histamine H
Jiangsu Marine Resources Development Research Institute
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
Jagiellonian University Medical College
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists.
University College London
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
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
Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.
Astrazeneca
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: high affinity and human/rat species-selective histamine H(3) receptor antagonists.
Osaka University of Pharmaceutical Sciences
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.
Zhejiang University
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.
United Arab Emirates University
Determination of the binding mode and interacting amino-acids for dibasic H3 receptor antagonists.
Bioprojet-Biotech
A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.
Schering-Plough Research Institute
Design of potent non-thiourea H3-receptor histamine antagonists.
University College London
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
Vrije Universiteit Amsterdam
Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold.
University of Parma
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Vrije Universiteit Amsterdam
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Vrije Universiteit
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.
Osaka University
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.
University of Kuopio
Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.
Vrije Universiteit
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Huazhong University of Science and Technology
Design, synthesis, and biological evaluation of novel oxadiazole- and thiazole-based histamine H
Heinrich Heine University D£Sseldorf
Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H
Jagiellonian University Medical College
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.
Novartis Institutes For Biomedical Research
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
Jagiellonian University Medical College
Identification of novel β-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents.
Csir-Central Drug Research Institute
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
Iqog, Csic
Novel naphthyloxy derivatives - Potent histamine H
Jagiellonian University Medical College
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
Vrije Universiteit
Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.
Novartis Institutes For Biomedical Research
Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.
Bioprojet-Biotech
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
FGFR4 inhibitor and preparation method and use thereof
Jiangsu Hansoh Pharmaceutical Group
A high quality, industrial data set for binding affinity prediction: performance comparison in different early drug discovery scenarios.
F. Hoffmann-La Roche
Method of treatment using substituted imidazo[1,2b]pyridazine compounds
Array Biopharma
Combination Alzheimer therapy using anti-N3pGlu Abeta antibodies + a BACE inhibitor
Eli Lilly
Substituted oxopyridine derivatives and use thereof as factor xia/plasma
Bayer Pharma Aktiengesellschaft
Anti-infective agents against intracellular pathogens
The Ohio State University Research Foundation
New tryptophanase inhibitors: towards prevention of bacterial biofilm formation.
Ben-Gurion University of The Negev
Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.
University of Tokyo
Characterisation of the melanocortin 4 receptor by radioligand binding.
Uppsala University
[3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Synaptic Pharmaceutical
Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.
University of California San Francisco
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
Merck Research Laboratories
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Thermodynamics of molecular recognition by cyclodextrins. 1. Calorimetric titration of inclusion complexation of naphthalenesulfonates with .alpha.-, .beta.-, and .gamma.-cyclodextrins: enthalpy-entropy compensation
Himeji Institute of Technology
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Bristol-Myers Squibb
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.
Nih
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Chemical Genomics Centre of The Max Planck Society
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.
Bristol-Myers Squibb
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
University of North Carolina At Chapel Hill