139 articles for thisTarget

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PMID	Data	Article Title	Organization
27997171	48	Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.	The University of Newcastle
12372505	120	Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.	Abbott Laboratories
12113835	176	Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.	Abbott Laboratories
27876250	60	Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH	Jagiellonian University Medical College
27839919	192	Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.	University of Kansas
27007611	115	Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.	University of Regensburg
26937601	55	Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.	Merck Research Laboratories
26988801	55	Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.	Jagiellonian University Medical College
26704965	229	Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.	University of Illinois At Chicago
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
26475518	19	Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.	City University of New York
25993395	19	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.	Janssen Research and Development
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.
24735492	98	Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.	Sanford-Burnham Medical Research Institute
24365159	35	The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.	University of Missouri
24269482	35	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.	Glaxosmithkline
23981939	32	N-substituted 8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes ass receptor ligands with potential neuroprotective effects.	The University of Sydney
23909910	177	Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists.	Emory University
23816046	8	Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates.	Columbia University Medical Center
23707254	7	Selectivity of phenothiazine cholinesterase inhibitors for neurotransmitter systems.	Dalhousie University
23602445	23	An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.	Ucl School of Pharmacy
23582449	20	Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.	Institute of Organic Synthesis
23466604	36	Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.	Universit£
23403082	28	Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.	Broad Institute of Mit and Harvard
23558237	17	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.	Griffin Discoveries
20409707	66	Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.	University of Regensburg
19791743	41	Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.	University of Regensburg
19317445	53	N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.	University of Regensburg
12657274	109	Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.	Abbott Laboratories
12113836	162	Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.	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
21486038	177	Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.	H. Lundbeck
23641311	38	From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.	TBA
22216892	66	The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.	University of Regensburg
22578490	35	Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.	Cephalon
22475308	3	Bis-spirolabdane diterpenoids from Leonotis nepetaefolia.	University of Mississippi
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
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
20931963	112	Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.	Aska Pharmaceutical
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
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
18950149	75	Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.	University of Regensburg
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
17483457	58	A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.	Abbott Laboratories
18077160	126	In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.	Abbott Laboratories
11585444	295	From hit to lead. Analyzing structure-profile relationships.	Universities of Lille
15203136	39	(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.	Virginia Commonwealth University
22153342	60	Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.	Cephalon
22014551	33	Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.	Cephalon
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
20800486	16	Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.	Neurocrine Biosciences
21381763	52	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.	Glaxosmithkline
21146989	46	Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.	The University of Sydney
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)
20591666	66	A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.	Università
20452213	65	Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.	Johnson & Johnson Pharmaceutical Research & Development
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
20137933	218	Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.	Amgen
19773175	41	2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.	Johann Wolfgang Goethe University
19646882	72	Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.	University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
19632840	43	Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.	Tsukuba Research Institute
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
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
19271735	35	Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).	Wyeth Research
19231180	81	Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.	Roche Palo Alto
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
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
18598020	75	Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.	Tsukuba Research Institute
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
16942032	64	Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.	Hokkaido University
16730977	2	Synthesis and pharmacological characterization of novel fluorescent histamine H2-receptor ligands derived from aminopotentidine.	The University of Kansas
16722655	28	Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.	Pfizer
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
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
16134937	154	6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.	7Tm Pharma
15634025	29	2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.	Novo Nordisk
15566302	101	Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.	RhôNe-Poulenc Rorer
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
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
12372500	108	Synthesis and evaluation of potent pyrrolidine H(3) antagonists.	Abbott Laboratories
32832018	34	Fluorescent H	University of Regensburg
32227883	40	Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge	University of Mississippi
32420741	134	UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H	University of Regensburg
10956183	19	De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.	Synaptic Pharmaceutical
30597325	17	Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (?	Memorial Sloan Kettering Cancer Center
32342685	325	Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D	National Institute of Neurological Disorders and Stroke
31021617	136	Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D	University of Pennsylvania
30998358	60	Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.	Academy of Scientific and Innovative Research (Acsir)
30875219	254	Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D	University of North Carolina At Chapel Hill
30605331	236	Design and in Vivo Characterization of A	Medical College of Wisconsin
31185168	144	Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.	Rti International
9857099	94	Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.	Synaptic Pharmaceutical
31469288	180	[	University of Regensburg
31620230	283	3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT	University of Minnesota Twin Cities
26236460	36	Structure-Based Design, Synthesis by Click Chemistry and	National Institute of Diabetes and Digestive and Kidney Diseases
26469213	58	Phenyl Ether- and Aniline-Containing 2-Aminoquinolines as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase.	Northwestern University
21075638	105	Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.	Drug Discovery Laboratory
21044842	206	Histamine H4 receptor agonists.	University of Regensburg
15771452	49	N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.	Vrije Universiteit Amsterdam
30389290	146	Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.	Texas Tech University Health Sciences Center
29767967	74	Structure-Guided Modification of Heterocyclic Antagonists of the P2Y	National Institute of Diabetes and Digestive and Kidney Diseases
29656199	148	Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.	University of Texas At Austin
29631962	252	Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.	Phenex Pharmaceuticals
28764962	90	Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel?	Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
28776992	110	Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.	Northwestern University
28636348	9	Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.	National Institute of Diabetes and Digestive and Kidney Diseases
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
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
3828800	17	The characterization of [3H]sulpiride binding sites in rat striatal membranes.	St, Marianna University School of Medicine