The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 12372505 |
120 |
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands. |
Abbott Laboratories |
| 27866818 |
84 |
The discovery of quinoline based single-ligand human H |
Glaxosmithkline |
| 27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University Of Kansas |
| 27692832 |
7 |
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists. |
Bioprojet-Biotech |
| 27584694 |
103 |
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 |
| 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. |
Novartis Institutes Of Biomedical Research (Nibr) |
| 27007611 |
115 |
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
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. |
Astrazeneca |
| 26390077 |
42 |
Tactical Approaches to Interconverting GPCR Agonists and Antagonists. |
University Of Minnesota |
| 26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
| 26731168 |
39 |
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists. |
Suven Life Sciences |
| 26718844 |
55 |
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity. |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
| 26690914 |
22 |
Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents. |
Jagiellonian University Medical College |
| 25993395 |
19 |
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators. |
Janssen Research And Development |
| 25893048 |
25 |
Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development. |
Janssen Pharmaceutical Companies Of Johnson & Johnson |
| 25941545 |
21 |
Biphenyl-ethyl-pyrrolidine derivatives as histamine h3 receptor modulators for the treatment of cognitive disorders. |
Temple University |
| 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. |
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. |
University Of Florida |
| 25047936 |
183 |
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode. |
Universit£T Regensburg |
| 25218907 |
18 |
Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs. |
University Of Catania |
| 24996140 |
26 |
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands. |
Jagiellonian University Medical College |
| 24745967 |
19 |
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness. |
Johann Wolfgang Goethe University |
| 24495018 |
77 |
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. |
Janssen Research And Development |
| 24650714 |
21 |
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties. |
United Arab Emirates University |
| 24900647 |
8 |
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand. |
Goethe University |
| 23218604 |
30 |
Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold. |
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. |
Vrije Universiteit Amsterdam |
| 22222138 |
40 |
Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain. |
Universit£ |
| 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. |
Vu University Amsterdam |
| 21348462 |
64 |
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. |
Vu University Amsterdam |
| 20409707 |
66 |
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity. |
University Of Regensburg |
| 20171098 |
20 |
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring. |
Abbott Laboratories |
| 19791743 |
41 |
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. |
University Of Regensburg |
| 19524331 |
33 |
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines. |
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. |
Vu University Amsterdam |
| 19317445 |
53 |
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
University Of Regensburg |
| 18976927 |
83 |
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity. |
Universit£ |
| 15771465 |
56 |
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
| 12657274 |
109 |
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. |
Abbott Laboratories |
| 23099096 |
88 |
Novel azulene derivatives for the treatment of erectile dysfunction. |
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). |
The University Of Sydney |
| 22483590 |
5 |
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) |
| 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). |
Pfizer |
| 22216892 |
66 |
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists. |
University Of Regensburg |
| 21062081 |
47 |
Histamine H3 receptor as a drug discovery target. |
TBA |
| 22985961 |
99 |
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
Glaxosmithkline |
| 24900450 |
44 |
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes. |
TBA |
| 22578490 |
35 |
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists. |
Cephalon |
| 22450133 |
64 |
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists. |
Cephalon |
| 22617490 |
23 |
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists. |
Cephalon |
| 22607684 |
50 |
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands. |
The University Of Sydney |
| 22464130 |
27 |
Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists. |
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. |
Pfizer |
| 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. |
National Institute Of Mental Health |
| 22444026 |
103 |
Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies. |
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. |
Cephalon |
| 21906941 |
94 |
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists. |
Cephalon |
| 21782432 |
62 |
Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity. |
Cephalon |
| 21824776 |
31 |
Amine-constrained pyridazinone histamine H3 receptor antagonists. |
Cephalon |
| 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. |
Cephalon |
| 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. |
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. |
H. Lundbeck |
| 20541426 |
46 |
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. |
Meiji Seika Kaisha |
| 20561786 |
77 |
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development. |
Johnson & Johnson Pharmaceutical Research & Development |
| 20299215 |
49 |
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. |
Argenta Discovery |
| 19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
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. |
F. Hoffmann-La Roche |
| 19091563 |
79 |
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
Johann Wolfgang Goethe Universit£T |
| 19329325 |
20 |
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands. |
Jagiellonian University Medical College |
| 18950149 |
75 |
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists. |
University Of Regensburg |
| 18606542 |
7 |
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists. |
F. Hoffmann-La Roche |
| 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. |
Purdue University |
| 18249544 |
12 |
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. |
Johnson & Johnson Pharmaceutical Research And Development |
| 18077160 |
126 |
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series. |
Abbott Laboratories |
| 18060777 |
158 |
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
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. |
Abbott Laboratories |
| 15139761 |
33 |
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists. |
Novo Nordisk |
| 12672253 |
60 |
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
Freie Universit£T Berlin |
| 12954048 |
36 |
The first potent and selective non-imidazole human histamine H4 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
| 12190321 |
55 |
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties. |
Freie Universit£T Berlin |
| 22326166 |
40 |
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists. |
Merck Research Laboratories |
| 22297111 |
32 |
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity. |
Cephalon |
| 22290075 |
60 |
4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity. |
Cephalon |
| 22197136 |
29 |
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists. |
Cephalon |
| 22189138 |
62 |
Synthesis of novel histamine H4 receptor antagonists. |
Pfizer |
| 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). |
Arena Pharmaceuticals |
| 22153663 |
59 |
Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics. |
Griffin Discoveries |
| 22153342 |
60 |
Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists. |
Cephalon |
| 22142542 |
73 |
4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists. |
Cephalon |
| 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. |
Zhejiang University |
| 22014551 |
33 |
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists. |
Cephalon |
| 22007643 |
25 |
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor. |
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). |
Pfizer |
| 21944855 |
30 |
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity. |
Cephalon |
| 21937153 |
46 |
Recent progress in synthesis and bioactivity studies of indolizines. |
University Of Botswana |
| 21843941 |
40 |
Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists. |
Pfizer |
| 21802950 |
466 |
Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. |
Bioprojet-Biotech |
| 21783360 |
52 |
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series. |
Bioprojet-Biotech |
| 19577344 |
43 |
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
| 21498080 |
45 |
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
Jagiellonian University Medical College |
| 21186123 |
36 |
Discovery of a series of potent arylthiadiazole H(3) antagonists. |
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. |
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. |
Universidad De Navarra |
| 20843691 |
26 |
Indole- and benzothiophene-based histamine H3 antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 20833043 |
28 |
Investigation of 4-piperidinols as novel H3 antagonists. |
Athersys |
| 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. |
F. Hoffmann-La Roche |
| 20728354 |
16 |
Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers. |
Johann Wolfgang Goethe University |
| 20727744 |
10 |
Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles. |
Johann Wolfgang Goethe University |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
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. |
Meiji Seika Kaisha |
| 20667729 |
86 |
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists. |
Evotec (Uk) |
| 20457525 |
225 |
In vitro studies on a class of quinoline containing histamine H3 antagonists. |
Abbott Laboratories |
| 20452213 |
65 |
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands. |
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. |
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. |
Meiji Seika Kaisha |
| 20382018 |
81 |
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 20188550 |
41 |
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists. |
Merck Research Laboratories |
| 19846299 |
52 |
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
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. |
Hokkaido University |
| 20042333 |
21 |
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists. |
Wyeth Research |
| 19632840 |
43 |
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists. |
Tsukuba Research Institute |
| 19773164 |
53 |
Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists. |
Schering-Plough Research Institute |
| 19524437 |
31 |
Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs. |
Hoffmann-La Roche |
| 19722526 |
30 |
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity. |
Arena Pharmaceuticals |
| 19520574 |
49 |
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists. |
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. |
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. |
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. |
Vanderbilt University |
| 18922693 |
37 |
2-Aryloxymethylmorpholine histamine H(3) antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 19329329 |
183 |
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 |
| 19286376 |
17 |
Fluorinated non-imidazole histamine H3 receptor antagonists. |
Johann Wolfgang Goethe-UniversitäT |
| 19119007 |
34 |
Novel imidazole-based histamine H3 antagonists. |
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. |
Tsukuba Research Institute |
| 18841880 |
82 |
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18783208 |
11 |
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 |
| 18774720 |
14 |
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands. |
Jagiellonian University Medical College |
| 18768318 |
37 |
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists. |
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. |
National Institute Of Mental Health |
| 18752952 |
31 |
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands. |
The Schering Plough Research Institute |
| 18598020 |
75 |
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18554904 |
26 |
Novel H3 receptor antagonists with improved pharmacokinetic profiles. |
Arena Pharmaceuticals |
| 18353639 |
27 |
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I. |
Kyowa Hakko Kogyo |
| 17918921 |
35 |
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists. |
Abbott Laboratories |
| 17616397 |
107 |
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 17583504 |
51 |
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 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. |
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. |
Glaxosmithkline |
| 17498953 |
17 |
A new class of histamine H3 receptor antagonists derived from ligand based design. |
F. Hoffmann-La Roche |
| 17412583 |
81 |
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity. |
Johnson & Johnson Pharmaceutical Research & Development |
| 17317177 |
69 |
Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors. |
Johnson & Johnson Pharmaceutical Research And Development |
| 17307358 |
81 |
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
| 17169555 |
46 |
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
Abbott Laboratories |
| 17127059 |
96 |
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. |
Johnson & Johnson Pharmaceutical Research And Development |
| 17107798 |
90 |
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore. |
Johnson & Johnson Pharmaceutical Research And Development |
| 16942032 |
64 |
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
Hokkaido University |
| 16908150 |
59 |
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides. |
Novo Nordisk |
| 16677814 |
67 |
Synthesis and SAR of novel histamine H3 receptor antagonists. |
Eli Lilly |
| 16616493 |
14 |
Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor. |
Novo Nordisk |
| 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. |
Columbia University College Of Physicians And Surgeons |
| 16434192 |
6 |
Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities. |
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. |
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. |
Johnson & Johnson Pharmaceutical Research And Development |
| 16300945 |
21 |
Aplysamine-1 and related analogs as histamine H3 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
| 16246552 |
57 |
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold. |
The Schering Plough Research Institute |
| 16190774 |
60 |
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
Abbott Laboratories |
| 15634025 |
29 |
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. |
Novo Nordisk |
| 15115409 |
72 |
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists. |
Freie UniversitäT Berlin |
| 14741270 |
152 |
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans. |
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. |
Abbott Laboratories |
| 12798320 |
64 |
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 |
| 12729661 |
20 |
Non-imidazole heterocyclic histamine H3 receptor antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
| 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. |
Hokkaido University |
| 12392739 |
41 |
Novel human histamine H(3) receptor antagonists. |
Johnson And Johnson Pharmaceutical Research And Development |
| 12182878 |
12 |
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors. |
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. |
Freie UniversitäT Berlin |
| 11294398 |
26 |
Different antagonist binding properties of human and rat histamine H3 receptors. |
Freie UniversitäT Berlin |
| 26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
| 26598975 |
16 |
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. |
University Of Toronto |
| 26685080 |
6 |
Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel. |
Novartis Institutes Of Biomedical Research Institute |
| 26851736 |
160 |
Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity. |
Panjab University |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University Of Leipzig |
| 7925364 |
13 |
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 |
| 4151898 |
13 |
Muscarinic cholinergic binding in rat brain. |
TBA |
| 3828800 |
17 |
The characterization of [3H]sulpiride binding sites in rat striatal membranes. |
St, Marianna University School Of Medicine |
| 16686531 |
26 |
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain. |
Mgi Pharma |
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