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342 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27876250 60 Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI Jagiellonian University Medical College
27639363 141 Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.EBI Huazhong University of Science and Technology
27866818 84 The discovery of quinoline based single-ligand human HEBI GlaxoSmithKline Medicines Research Centre
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27643714 26 Identification of Ligand Binding Hot Spots of the Histamine HEBI Vrije Universiteit Amsterdam
27717652 275 Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI Florida A&M University
27364609 230 Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.EBI Florida A&M University
27312422 219 Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.EBI Florida A&M University
27173799 97 Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.EBI Shanghai Institute of Materia Medica
27007611 115 Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI University of Regensburg
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.EBI Jagiellonian University Medical College
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26718844 55 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.EBI Friedrich-Alexander-Universit£t Erlangen-N£rnberg
26483200 100 Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.EBI Huazhong University of Science and Technology
25993395 19 Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI Janssen Research& Development, LLC
26191365 49 Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.EBI Novartis Institutes for BioMedical Research
25494650 8 CNS drug design: balancing physicochemical properties for optimal brain exposure.EBI Eli Lilly and Company
25827402 54 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.EBI Teva Global R&D.
25557493 109 Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI Jagiellonian University Collegium Medicum
25070422 126 Further evaluation of the tropane analogs of haloperidol.EBI Florida A&M University
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
25343529 221 Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.EBI Universit£ degli Studi di Siena
25318072 48 Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.EBI Max Planck Institute of Psychiatry
24805037 380 Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI Adamed Ltd.
24800940 146 Identification of a new selective dopamine D4 receptor ligand.EBI Florida A&M University
24690494 92 Antagonists of the kappa opioid receptor.EBI The Scripps Research Institute
24559051 141 Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.EBI Intra-Cellular Therapies, Inc.
24650714 21 Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.EBI United Arab Emirates University
24487191 6 Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.EBI Huazhong University of Science and Technology
24365159 35 The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.EBI University of Missouri
24269482 35 Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.EBI GlaxoSmithKline R&D
24161834 17 The discovery of the benzazepine class of histamine H3 receptor antagonists.EBI GlaxoSmithKline R&D
24147864 6 Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).EBI National Institute of Mental Health
23919353 8 Polypharmacology - foe or friend?EBI F. Hoffmann-La Roche Ltd.
24035337 10 2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.EBI Virginia Commonwealth University
23981939 32 N-substituted 8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes ass receptor ligands with potential neuroprotective effects.EBI The University of Sydney
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.EBI Columbia University Medical Center
23707254 7 Selectivity of phenothiazine cholinesterase inhibitors for neurotransmitter systems.EBI Dalhousie University
23602445 23 An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.EBI UCL School of Pharmacy
23591112 4 Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II).EBI Sanofi US
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.EBI Institute of Organic Synthesis
23466604 36 Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.EBI Universit£ degli Studi di Siena
23403082 28 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.EBI Broad Institute of MIT and Harvard
23675993 13 Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.EBI Huazhong University of Science and Technology
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.EBI Griffin Discoveries BV
14667234 23 Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.EBI Vrije Universiteit Amsterdam
12443779 30 2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI Johnson& Johnson Pharmaceutical Research& Development
 3 Optical isomers of the H1 antihistamine terfenadine: synthesis and activityEBI TBA
21944853 41 Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.EBI University of Regensburg
20674357 66 Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.EBI GlaxoSmithKline
16408006 3 Linking agonist binding to histamine H1 receptor activation.EBI Vrije Universiteit Amsterdam
20409707 66 Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.EBI University of Regensburg
19791743 41 Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.EBI University of Regensburg
19524331 33 Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.EBI Johnson& Johnson Pharmaceutical Research& Development
18990469 23 Non-imidazole histamine H3 ligands, part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.EBI Medical University
19317445 53 N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.EBI University of Regensburg
19053770 68 Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.EBI Vrije Universiteit Amsterdam
18248991 323 New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.EBI GlaxoSmithKline
14640554 31 N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.EBI Freie Universit£t Berlin
10737740 57 Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.EBI Freie Universit£t Berlin
9548813 53 The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI SmithKline Beecham Pharmaceuticals
7650688 6 The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor.EBI Vrije Universiteit
1977909 36 Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines. A new class of potent H1 antagonists.EBI Central Drug Research Institute
2569042 36 Synthesis and in vitro pharmacology of arpromidine and related phenyl(pyridylalkyl)guanidines, a potential new class of positive inotropic drugs.EBI Freie Universit£t Berlin
6121914 2 1,2,5-thiadiazole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists.EBI TBA
12657274 2 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott Laboratories
12657255 21 Synthesis and pharmacological activity of fluorescent histamine H1 receptor antagonists related to mepyramine.EBI Peking University
11755365 119 Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.EBI Janssen-Cilag
11755364 107 Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.EBI Janssen-Cilag
12113836 1 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.EBI Abbott Laboratories
9873585 30 N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.EBI Freie Universit£t Berlin
23142617 57 Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I.EBI AstraZeneca
23116889 88 Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: optimising in vivo clearance.EBI AstraZeneca
23099096 88 Novel azulene derivatives for the treatment of erectile dysfunction.EBI Friedrich Alexander University
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI 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.EBI H. Lundbeck A/S
23009245 53 Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI Sanford-Burnham Medical Research Institute
23006002 35 Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.EBI Suven Life Sciences Ltd.
22931505 69 Chemokine receptor antagonists.EBI National Heart and Lung Institute
23031591 90 The discovery of CCR3/H1 dual antagonists with reduced hERG risk.EBI AstraZeneca
22793499 19 Shape-based reprofiling of FDA-approved drugs for the H1 histamine receptor.EBI University of Oxford
22694093 16 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI National Institute of Biological Sciences
23021991 153 Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.EBI AstraZeneca
22985961 99 Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
22578490 35 Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22520153 135 Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.EBI Florida A&M University
22313242 146 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI Pfizer Inc.
22313227 78 Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.EBI National Institute of Mental Health
21207959 69 Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI National Institute of Mental Health
20875743 90 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 relaEBI Pfizer Inc.
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.EBI ASKA Pharmaceutical Co, Ltd
20684563 176 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI H. Lundbeck A/S
20541426 46 Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI Meiji Seika Kaisha, Ltd
20299215 49 Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.EBI Argenta Discovery Ltd.
20188547 152 Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
19963380 38 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI Hunter College and the Graduate Center of the City University of New York
17846138 26 Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.EBI Veterans Affairs Medical Center
19091563 79 Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.EBI Johann Wolfgang Goethe Universit£t
18950149 75 Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI University of Regensburg
16562853 22 Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.EBI Tom's of Maine
18468904 48 High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI Purdue University
17360666 7 From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.EBI The Johns Hopkins University School of Medicine
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18077160 126 In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI Abbott Laboratories
18023344 77 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.EBI F. Hoffmann-La Roche Ltd
17998160 101 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI F. Hoffmann-La Roche Ltd
18052318 30 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.EBI GlaxoSmithKline Medicines REsearch Centre
17407815 27 Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.EBI Johnson& Johnson Pharmaceutical Research& Development
17267226 46 Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity.EBI Taisho Pharmaceutical Co., Ltd
16821797 21 (R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.EBI Mitsubishi Pharma Corporation
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15771458 5 Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.EBI Johnson& Johnson Pharmaceutical Research& Development
14998318 112 Selective optimization of side activities: another way for drug discovery.EBI Prestwick Chemical Inc.
12672253 60 Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.EBI Freie Universit£t Berlin
12747773 13 Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.EBI Aventis Pharmaceuticals
11784139 82 Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.EBI Universit£ degli Studi di Siena
12213075 70 Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).EBI Purdue University
12190321 55 Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.EBI Freie Universit£t Berlin
11170639 73 Current and novel approaches to the drug treatment of schizophrenia.EBI Merck Sharp and Dohme
11708905 20 N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.EBI Lilly Research Laboratories
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI F-59000 Lille
10447960 20 Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.EBI Universidad de Valencia
9703460 52 Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.EBI National Taiwan University
9083484 84 New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI Cooperation Pharmaceutique Fran�aise
7562938 17 New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.EBI Wyeth-Ayerst Research
1353796 33 Synthesis and antihistaminic activity of some thiazolidin-4-ones.EBI Universit£ di Napoli Federico II
1350797 21 Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives.EBI Kyowa Hakko Kogyo Co., Ltd.
1908521 37 Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.EBI Centre de Recherches de Vitry Alfortville Rh£ne-Poulenc Rorer
2879912 55 Synthesis of 2-(4-substituted-1-piperazinyl)benzimidazoles as H1-antihistaminic agents.EBI TBA
2869146 35 Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.EBI TBA
15203136 37 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
 52 Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activityEBI TBA
 24 1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonistsEBI TBA
14695828 96 Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.EBI Universit£ degli Studi di Siena
22336245 72 Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.EBI Florida A&M University
22245230 128 Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI Florida A&M University
22153663 59 Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.EBI Griffin Discoveries BV
22153347 111 Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia.EBI Neurocrine Biosciences
22153342 60 Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22014551 33 Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI Cephalon, Inc.
22007643 25 Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.EBI VU University Amsterdam
21955944 39 Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).EBI Pfizer Inc.
21788137 33 N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI The University of Sydney
20800486 16 Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences
19443217 60 Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.EBI Chemical Diversity Research Institute
21555222 25 Molecular hybridization of 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (s) receptor ligands modulates off-target activity and subtype selectivity.EBI The University of Sydney
21498080 45 N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.EBI Jagiellonian University Medical College
21470866 21 Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.EBI Dainippon Sumitomo Pharma. Co., Ltd
21381763 52 The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.EBI GlaxoSmithKline Medicines Research Centre
21232954 75 Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.EBI Neurocrine Biosciences
21146989 46 Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI The University of Sydney
20942472 88 Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.EBI GlaxoSmithKline
20857909 176 Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.EBI University of Copenhagen
20812727 157 Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI National Institute of Mental Health
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20690643 68 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI Meiji Seika Kaisha, Ltd.
20667729 86 Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI Evotec (UK) Ltd
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
20452213 65 Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI 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.EBI Meiji Seika Kaisha, Ltd.
20347297 61 The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.EBI Neurocrine Biosciences
20227880 144 Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
20153647 6 The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.EBI GlaxoSmithKline
19786348 261 Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.EBI F. Hoffmann-La Roche Ltd
20045641 9 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.EBI Virginia Commonwealth University
20170186 49 1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.EBI GlaxoSmithKline Medicine Research Centre
19945877 50 Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.EBI Chemical Diversity Research Institute
19773175 41 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.EBI Johann Wolfgang Goethe-University
19646882 72 Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and the Informatics Institute of UMDNJ
19773162 72 Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.EBI Arena Pharmaceuticals
19660947 24 Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.EBI The Schering Plough Research Institute
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19553115 96 Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
19663387 29 Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences
19520574 49 Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI Tsukuba Research Institute
19362477 24 Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists.EBI Dainippon Sumitomo Phrama. Co. Ltd
19553110 16 Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.EBI Tsukuba Research Institute
 76 Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activityEBI TBA
 12 The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI TBA
 41 5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI TBA
 22 The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.EBI TBA
 20 Dual antagonists of platelet activating factor and histamine. 2. pyridine ring substitution of N-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidinesEBI TBA
19329329 183 Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
19072656 110 Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.EBI University of Siena
18952421 60 Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18841880 82 Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18817368 57 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI Merck Research Laboratories
18783208 11 Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI National Institute of Mental Health
18768318 37 Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc.
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18595716 142 Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.EBI Florida A&M University
18020391 12 From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.EBI F. Hoffmann-La Roche Ltd.
18020390 37 Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.EBI F. Hoffmann-La Roche Ltd.
17976986 80 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI Pfizer Global 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.EBI National Institute of Mental Health
17524641 69 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI GlaxoSmithKline
17328523 36 Novel sigma receptor ligands: synthesis and biological profile.EBI University of Catania
17234422 118 Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.EBI Taisho Pharmaceutical Co., Ltd
16942032 64 Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI Hokkaido University
16621538 35 Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.EBI Florida A& M University
16458504 37 Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI Columbia University College of Physicians and Surgeons
16392798 46 Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI Columbia University College of Physicians and Surgeons
16246552 57 Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.EBI The Schering Plough Research Institute
16143528 213 Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI 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.EBI 7TM Pharma A/S
15771448 187 Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI Johnson & Johnson Pharmaceutical Research & Development
15771415 155 Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI Johnson & Johnson Pharmaceutical Research & Development
15745824 1 Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.EBI Roche Palo Alto
15686934 20 Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.EBI Rhône-Poulenc Rorer
15686917 21 5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.EBI UCB Research
15634025 29 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI Novo Nordisk A/S
15566302 101 Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.EBI Rhône-Poulenc Rorer
15482930 22 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.EBI UCB Research
15125929 66 Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research & Development
15115409 72 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.EBI Freie Universität Berlin
15081022 18 5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.EBI UCB Research
14741266 203 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.EBI Abbott Laboratories
12798320 12 A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.EBI Abbott Laboratories
12781173 28 Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.EBI The Schering-Plough Research Institute
12723960 58 Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.EBI Hokkaido University
12372500 108 Synthesis and evaluation of potent pyrrolidine H(3) antagonists.EBI Abbott Laboratories
11934576 82 Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.EBI Université de Lille 2
11855993 91 Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.EBI Freie Universität Berlin
11784148 81 Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI Pharmazeutisches Institut der Universität Freiburg
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
10966752 60 New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.EBI Freie Universität Berlin
10956183 19 De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.EBI Synaptic Pharmaceutical Corporation
10937710 81 Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI Merck & Co.
10866399 10 Conformationally-restricted ligands for the histamine H1 receptor.EBI University of Bath
10841797 110 Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI The R.W. Johnson Pharmaceutical Research Institute
10464021 59 N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.EBI Knoll Pharmaceuticals
10377229 107 New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI University of Göteborg
9934454 15 Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.EBI Schering-Plough Research Institute
9873505 48 Novel H3 receptor antagonists. Sulfonamide homologs of histamine.EBI Schering-Plough Research Institute
9871662 15 Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.EBI Schering-Plough Research Institute
9857099 94 Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.EBI Synaptic Pharmaceutical Corporation
9406603 49 Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI University of Groningen
8709107 99 Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.EBI Yamanouchi Pharmaceutical Company Limited
8676353 140 Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.EBI Freie Universität Berlin
8246239 71 Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI Solvay Duphar B.V.
8093908 15 Dibenz[b,e]oxepin derivatives: novel antiallergic agents possessing thromboxane A2 and histamine H1 dual antagonizing activity. 1.EBI Kyowa Hakko Kogyo Co.
7752184 12 A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.EBI Schering-Plough Research Institute
7608912 6 (Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.EBI Vrije Universiteit
3746815 4 In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.EBI TBA
2562852 6 Synthesis and antiallergy activity of 4-(diarylhydroxymethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.EBI A.H. Robins Company
1681106 27 Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.EBI Pfizer Inc.
1673158 9 Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines.EBI A. H. Robins Company, Inc.
1671420 49 Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.EBI Schering-Plough Corporation
19337725 43 Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.BDB Case Western Reserve University
18387300 90 Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.BDB Pfizer Global Research and Development
17221184 55 Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.BDB Columbia University
16915381 31 WAY-100635 is a potent dopamine D4 receptor agonist.BDB Purdue University
16675639 28 Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.BDB Wyeth Research
16554355 47 N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.BDB University of Kansas
16352709 44 Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.BDB McGill University
15999145 62 Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.BDB Case Western Reserve University
15831442 46 Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.BDB Taisho Pharmaceutical Co., Ltd
15798001 56 Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.BDB Kyowa Hakko Kogyo Co., Ltd.
15608078 35 Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.BDB Abbott Laboratories
15169829 3 Ligand-directed functional heterogeneity of histamine H1 receptors: novel dual-function ligands selectively activate and block H1-mediated phospholipase C and adenylyl cyclase signaling.BDB University of North Carolina at Chapel Hill
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
15033391 33 Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.BDB Abbott Laboratories
12784105 53 Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.BDB Case Western Reserve University
12761331 97 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.BDB Case Western Reserve University
12721338 61 N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.BDB Pudue Pharma Discovery Research
12649361 779 L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.BDB Case Western Reserve University
12649305 4 Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).BDB Schering-Plough Research Institute
12629531 203 H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.BDB Case Western Reserve University
12626648 19 Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.BDB University of Kansas
12606603 59 Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.BDB Abbott Laboratories
12527336 21 Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.BDB Aventis Pharma
12431845 84 Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.BDB Lilly Research Laboratories
12388666 301 Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.BDB Institut de Recherches Servier
12232544 79 [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine].BDB Emory University
12192085 52 Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.BDB Case Western Reserve University
12110997 380 In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.BDB Westfälische Wilhelms-Universitä Muenster,
12065734 57 A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.BDB University of North Carolina at Chapel Hill
11809864 10 Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).BDB UCB S.A.
11750180 139 Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.BDB Lilly Research Laboratories
11438309 51 The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.BDB Janssen Research Foundation
11132243 125 Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds.BDB Mayo Foundation for Medical Education and Research and Mayo Clinic
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
10379421 134 Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.BDB TBA
10227113 22 Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.BDB Lilly Research Laboratories
9454810 72 SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB Sanofi Recherche
9430133 176 Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.BDB H. Lundbeck A/S
9400006 184 Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.BDB Emory University
9395253 17 Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.BDB Eli Lilly and Co.
9336327 37 The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.BDB Preclinical R & D, Astra Arcus AB
9144661 24 BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.BDB SmithKline Beecham Pharmaceuticals
8996185 121 Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.BDB Synthélabo Recherche
8968364 10 Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist.BDB Pharmacia and Upjohn, Inc.
8935801 586 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.BDB Janssen Research Foundation
8903934 7 Pharmacological and functional characterisation of the wild-type and site-directed mutants of the human H1 histamine receptor stably expressed in CHO cells.BDB Universite Libre de Bruxelles
8822531 111 Radioreceptor binding profile of the atypical antipsychotic olanzapine.BDB Lilly Research Laboratories
8821530 16 In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.BDB SmithKline Beecham Pharmaceuticals
8788493 64 Novel discriminatory ligands for 5-HT2B receptors.BDB SmithKline Beecham Pharmaceuticals
8730737 23 Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.BDB SmithKline Beecham Pharmaceuticals
8584042 40 BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex.BDB Boehringer Ingelheim Italia
8564266 77 Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.BDB Vrije Universiteit
8335064 4 Characteristics of histamine H1 receptors on HeLa cells.BDB University of Cambridge
8093723 20 Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties.BDB Dainippon Pharmaceutical Co., Ltd.
8012715 38 GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.BDB Glaxo Group Research Ltd.
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.BDB Université Libre de Bruxelles
7910212 34 Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.BDB Yamanouchi Pharmaceutical Co. Ltd.
7855217 139 Binding of antidepressants to human brain receptors: focus on newer generation compounds.BDB Mayo Clinic Jacksonville
7523657 14 Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity.BDB Eli Lilly and Company
7518514 46 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.BDB Abbott Laboratories
6149136 83 Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.BDB Mayo Clinic and Foundation
6146381 35 Histamine H1 receptors in human brain labelled with [3H]doxepin.BDB Mayo Foundation
6123593 24 A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain.BDB Eli Lilly and Company
3790168 23 Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative.BDB Wyeth Laboratories, Inc.
3419539 56 Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers.BDB Organon International
2904784 109 Neuroleptic binding to human brain receptors: relation to clinical effects.BDB Mayo Clinic and Foundation
2869639 166 Effects of remoxipride and some related new substituted salicylamides on rat brain receptors.BDB Astra Läkemedel AB
2530094 94 The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.BDB Novo Industri A/S
1982626 30 Neurochemical profile of eltoprazine.BDB Duphar B.V.
1661335 95 Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.BDB Center for Bio-Pharmaceutical Sciences
1501121 12 Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist.BDB Sanofi Recherche
1321744 14 Multiple histamine receptors: properties and functional characteristics.BDB Queen's Medical Centre
282646 50 Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine.BDB TBA
19700330 36 Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.BDB Virginia Commonwealth University
18683917 57 The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.BDB Abbott Laboratories
18983139 12 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia.BDB Abbott Laboratories
14722321 9 A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.BDB Johnson & Johnson Pharmaceutical