113 articles for BL Roth
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
35
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.
University of Illinois At Chicago
28
A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.
Virginia Commonwealth University
20
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Florida A&M University
18
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.
Florida A&M University
23
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
24
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.
Massachusetts General Hospital
42
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
University of Illinois At Chicago
25
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.
University of Mississippi
34
Identification of a new selective dopamine D4 receptor ligand.
Florida A&M University
30
Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor.
Institute of Science and Technology
1
Discovery ofβ2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
University of Dundee
12
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
University of North Carolina at Chapel Hill
2
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School of Pharmacy
6
Colloidal aggregation causes inhibition of G protein-coupled receptors.
University of North Carolina at Chapel Hill
38
Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists.
University of North Carolina at Chapel Hill
12
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.
University of Li£Ge
3
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
National Institute of Biological Sciences
10
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.
University of North Carolina at Chapel Hill
23
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Florida A&M University
15
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.
TBA
25
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.
Virginia Commonwealth University
27
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.
University of Milan
21
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.
Virginia Commonwealth University
16
Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Virginia Commonwealth University
7
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors.
Florida A&M University
12
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.
Florida A&M University
23
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
Florida A&M University
3
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.
University of Mississippi
12
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
University of North Carolina at Chapel Hill
47
Design, synthesis, and subtype selectivity of 3,6-disubstitutedß-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
University of Wisconsin-Milwaukee
12
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
Csiro Molecular and Health Technologies
5
9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.
Virginia Commonwealth University
147
Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.
St. Jude Children'S Hospital
68
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
University of Illinois At Chicago
20
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
Florida A&M University
5
Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.
Virginia Commonwealth University
16
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.
Florida A&M University
53
D4 dopamine receptor high-resolution structures enable the discovery of selective agonists.
University of North Carolina at Chapel Hill
11
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
UNC Eshelman School of Pharmacy
3
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Icahn School Of Medicine At Mount Sinai
12
Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.
Virginia Commonwealth University
4
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
University of Mississippi
16
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.
Faculté
31
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.
Université
23
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.
Virginia Commonwealth University
8
Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.
Virginia Commonwealth University
18
Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
6
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
2
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.
Florida A&M University
59
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
University of Illinois At Chicago
9
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
11
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
14
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
Virginia Commonwealth University
15
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.
Columbia University College of Physicians and Surgeons
36
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
Yale University
13
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
University of Melbourne
21
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
University of Health Sciences & Pharmacy At St. Louis
11
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Virginia Commonwealth University
15
Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.
Virginia Commonwealth University
19
Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
Virginia Commonwealth University
43
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
University of Illinois At Chicago
11
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College of Physicians and Surgeons
5
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
Georgetotwn University
14
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
Virginia Commonwealth University
16
Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.
Virginia Commonwealth University
15
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Virginia Commonwealth University
21
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Virginia Commonwealth University
45
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina at Chapel Hill
15
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
University of Illinois At Chicago
10
4β-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4β-methyl-5-(3-hydroxyphenyl)morphan pure antagonist.
Research Triangle Institute
3
1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist.
Purdue University
18
Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.
University of Mississippi
6
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
49
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets.
University of California San Francisco
25
Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor.
University of Southern California
3
Combination of a selective histone deacetylase 3 (HDAC3) inhibitor and an immunotherapy agent for the treatment of cancer
Kdac Therapeutics
46
SUBSTITUTED PYRROLO[2,3-D]PYRIMIDINES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
Sanofi
25
C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
18
Specific inhibitors of cytochrome P450 26 retinoic acid hydroxylase
University of Washington Through Its Center For Commercialization
2
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.
University of Sheffield
16
Design, synthesis and selection of DNA-encoded small-molecule libraries.
Praecis Pharmaceuticals
6
Impact of linker strain and flexibility in the design of a fragment-based inhibitor.
Johns Hopkins University
15
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
2
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
33
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
15
Thermodynamics of the molecular and chiral recognition of cycloalkanols and camphor by modified beta-cyclodextrins possessing simple aromatic tethers.
Nankai University
19
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
70
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
35
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Wyeth Research
34
Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase.
Shanghai Institutes For Biological Sciences
10
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.
Rutgers University
31
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bristol Myers Squibb
65
Rhodanine derivatives as selective protease inhibitors against bacterial toxins.
Burnham Institute For Medical Research