88 articles for AP Ijzerman
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A
Leiden University
5'-Substituted Amiloride Derivatives as Allosteric Modulators Binding in the Sodium Ion Pocket of the Adenosine A2A Receptor.
Leiden University
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
Leiden University
Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study.
University of Ferrara
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers.
Leiden University
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Leiden University
Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives.
TBA
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.
University of Ferrara
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.
Leiden University
Quantitative evaluation of the beta 2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolamines.
TBA
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Leiden University
Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Leiden University
A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor.
Center For Bio-Pharmaceutical Sciences
Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines.
TBA
Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data.
Leiden/Amsterdam Center For Drug Research
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.
Radboud University Nijmegen Medical Centre
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.
Leiden University
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.
Leiden University
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Leiden/Amsterdam Center For Drug Research
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.
Leiden University
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
University of Leiden
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Leiden University
Pyrazole derivatives as partial agonists for the nicotinic acid receptor.
Leiden/Amsterdam Center For Drug Research
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Leiden/Amsterdam Center For Drug Research
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
Vrije Universiteit
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
Leiden/Amsterdam Center For Drug Research
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
University of Camerino
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
Leiden/Amsterdam Center For Drug Research
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Leiden University
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.
University of Ghent
N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors.
Leiden/Amsterdam Center For Drug Research
Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor.
Leiden University
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Center For Bio-Pharmaceutical Sciences
Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
Vrije Universiteit
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.
University of Amsterdam
Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).
Leiden University
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists.
The Scripps Research Institute
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
Leiden University
Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.
Leiden University
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase.
Leiden/Amsterdam Center For Drug Research
Interference of linoleic acid fraction in some receptor binding assays.
Leiden University
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Leiden University
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
Leiden University
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A
Leiden University
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.
Leiden University
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.
Leiden Academic Centre For Drug Research
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Instituto De QuíMica MéDica (Csic)
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
Ghent University
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Leiden/Amsterdam Center For Drug Research
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Vrije Universiteit
Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength.
Heptares Therapeutics
Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.
Leiden/Amsterdam Center For Drug Research
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A
Leiden University
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.
Leiden University
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Vrije Universiteit
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Vrije Universiteit
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
National Institute of Diabetes
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.
Leiden University
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
Solvay Pharma
Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.
Leiden University
Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel.
Leiden University
Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists.
Leiden University
Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues.
Leiden University
N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands.
Solvay Duphar Research Laboratories
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
Leiden/Amsterdam Center For Drug Research
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties.
Center For Bio-Pharmaceutical Sciences
Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.
Leiden University
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
Center For Bio-Pharmaceutical Sciences
Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists.
Leiden University
Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A
Leiden University
Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold.
Nanchang University School of Pharmaceutical Science
Rationally designed sulfamides as glutamate carboxypeptidase II inhibitors.
Washington State University At Pullman
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Pfizer