Research Output per year
Research Output 1985 2014
- 1 - 50 out of 238 results
- Publication Year, Title (descending)
2014
The Receptor Concept in 3D: From Hypothesis and Metaphor to GPCR–Ligand Structures
Kooistra, A. J., de Graaf, C. & Timmerman, H., 2014, In : Neurochemical research. 39, 10, p. 1850-1861 12 p.Research output: Contribution to Journal › Article › Academic › peer-review
Metaphor
G-Protein-Coupled Receptors
Allosteric Site
Pharmaceutical Chemistry
Crystal structure
2010
Design, synthesis and pharmacological evaluation of non-peptidergic ligands for the human CXCR3 receptor
Storelli, S., 2010Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
Open Access
File
Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker
Wijtmans, M., Denonne, F., Célanire, S., Gillard, M., Hulscher, T. M., Delaunoy, C., Van Houtvin, N., Bakker, R. A., Defays, S., Gérard, J., Grooters, L., Hubert, D., Timmerman, H., Leurs, R., Talaga, P., De Esch, I. J. & Provins, L., 2010, In : MedChemComm. 1, p. 39-44Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H3 Receptors
Histamine Agonists
Ligands
2009
Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists
Celanire, S., Wijtmans, M., Christophe, B., Collart, P., de Esch, I. J. P., Dassesse, D., Delaunoy, C., Denonne, F., Durieu, V., Gelens, E., Gillard, M., Lallemand, B., Lamberty, Y., Lebon, F., Nicolas, J. M., Quere, L., Snip, E., Vanbellinghen, A., Van Houtvin, N., Verbois, V. & 4 others, 2009, In : ChemMedChem. 4, 7, p. 1063-8Research output: Contribution to Journal › Article › Academic › peer-review
Medicinal chemistry teaching and training: a continuous adaptation
Timmerman, H. & de Souza, N. J., 2009, In : ChemMedChem. 4, 7, p. 1055-8Research output: Contribution to Journal › Article › Academic › peer-review
Pharmaceutical Chemistry
Teaching
Obituary: To the Memory of Roelof Rekker
Timmerman, H. & Mannhold, R., 2009, In : QSAR and Combinatorial Science. 28, 5, p. 507-507Research output: Contribution to Journal › Article › Academic › peer-review
2008
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists
Wijtmans, M., Celanire, S., Snip, E., Gillard, M. R., Gelens, E., Collart, P. P., Venhuis, B. J., Christophe, B., Hulscher, ST., van der Goot, H., Lebon, F., Timmerman, H., Bakker, R. A., Leurs, R., Lallemand, B. I., Talaga, P. & de Esch, I. J. P., 2008, In : Journal of Medicinal Chemistry. 51, 10, p. 2944-53Research output: Contribution to Journal › Article › Academic › peer-review
Histamine Agonists
Imidazoles
Therapeutic Human Experimentation
Histamine
Constitutively active mutants of the histamine H1 receptor suggest a conserved hydrophobic asparagine-cage that constrains the activation of class A G protein-coupled receptors
Bakker, R. A., Jongejan, A., Sansuk, K., Hacksell, U., Timmerman, H., Brann, M. R., Weiner, D. M., Pardo, L. M. & Leurs, R., 2008, In : Molecular Pharmacology. 73, 1, p. 94-103Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H1 Receptors
Asparagine
G-Protein-Coupled Receptors
Histamine
2007
In vitro pharmacology of clinically used central nervous system-active drugs as inverse H(1) receptor agonists
Bakker, R. A., Nicholas, M. W., Smith, T. F., Burstein, E. S., Hacksell, U., Timmerman, H., Leurs, R., Brann, M. R. & Weiner, D. M., 2007, In : The Journal of Pharmacology and Experimental Therapeutics. 322, 1, p. 172-9Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
Central Nervous System Agents
Histamine
Pharmacology
In Vitro Techniques
Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity
Smit, M. J., Vischer, H. F., Bakker, R. A., Jongejan, A., Timmerman, H., Pardo, L. M. & Leurs, R., 2007, In : Annual Review of Pharmacology and Toxicology. 47, p. 53-87Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
G-Protein-Coupled Receptors
Structural analysis
Proteins
Pharmacogenetics
Point Mutation
Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists
Storelli, S., Verzijl, D., Al-Badie, J., Elders, N., Bosch, L., Timmerman, H., Smit, M. J., De Esch, I. J. & Leurs, R., 2007, In : Archiv der Pharmazie. 340, 6, p. 281-91Research output: Contribution to Journal › Article › Academic › peer-review
CXCR3 Receptors
Structure-Activity Relationship
Ligands
G-Protein-Coupled Receptors
4-hydroxyquinazoline
The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons
Dai, H., Fu, Q., Shen, Y., Hu, W., Zhang, Z., Timmerman, H., Leurs, R. & Chen, Z., 2007, In : European Journal of Pharmacology. 563, 1-3, p. 117-23Research output: Contribution to Journal › Article › Academic › peer-review
2006
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function
Govoni, M., Lim, H. D., El-Atmioui, D., Menge, W. M. P. B., Timmerman, H., Bakker, R. A., Leurs, R. & De Esch, I. J., 2006, In : Journal of Medicinal Chemistry. 49, 8, p. 2549-57Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H3 Receptors
Histamine
Gamma-herpesvirus-encoded G-protein-coupled receptors
Verzijl, D., 2006Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
Helix 8 of the viral chemokine receptor ORF74 directs chemokine binding
Verzijl, D., Pardo, L. M., van Dijk, M. A., Gruijthuijsen, Y. K., Jongejan, A., Timmerman, H., Nicholas, J., Schwarz, M., Murphy, P. M., Leurs, R. & Smit, M. J., 2006, In : Journal of Biological Chemistry. 281, 46, p. 35327-35Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
File
Human Herpesvirus 8
Chemokine Receptors
Chemokines
Chemokine CXCL1
Binding Sites
Histamine protects against NMDA-induced necrosis in cultured cortical neurons through H receptor/cyclic AMP/protein kinase A and H receptor/GABA release pathways
Dai, H., Zhang, Z., Zhu, Y., Shen, Y., Hu, W., Huang, Y. W., Luo, J., Timmerman, H., Leurs, R. & Chen, Z., 2006, In : Journal of Neurochemistry. 96, 5, p. 1390-400Research output: Contribution to Journal › Article › Academic › peer-review
Mutational analysis of the human histamine H1 receptor
Bruysters, MWP., 2006Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
2005
Isolation and structure elucidation of tracheospasmolytic compounds from piper cubeba l.f fruits and their possibility as anti-inslammatory activity
Wahyono, Z., 2005Research output: PhD Thesis › PhD Thesis - Research external, graduation external › Academic
Isolation and structure elucidation of tracheospasmolytic compounds from vitex trifolia l. leaves
Alam, G., 2005Research output: PhD Thesis › PhD Thesis - Research external, graduation external › Academic
New high affinity H3 receptor agonists without a basic side chain
Kitbunnadaj, R., Hoffmann, M., Fratantoni, S. A., Bongers, G. M., Bakker, R. A., Wieland, K., el Jilali, A., De Esch, I. J., Menge, W. M. P. B., Timmerman, H. & Leurs, R., 2005, In : Bioorganic and Medicinal Chemistry. 13, 23, p. 6309-23Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H3 Receptors
Histamine Agonists
Histamine
Amines
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist
Kitbunnadaj, R., Hashimoto, T., Poli, E., Zuiderveld, O. P., Menozzi, A., Hidaka, R., de Esch, I. J. P., Bakker, R. A., Menge, W. M. P. B., Yamatodani, A., Coruzzi, G., Timmerman, H. & Leurs, R., 2005, In : Journal of Medicinal Chemistry. 48, 6, p. 2100-7Research output: Contribution to Journal › Article › Academic › peer-review
Histamine Agonists
Imidazoles
Histamine
methimepip
Synthesis and In Vitro Pharmacological Evaluation of Novel Ligands for Histamine Receptors
Govoni, M., 2005Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
Open Access
File
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists
Storelli, S., Verdijk, P. W., Verzijl, D., Timmerman, H., van de Stolpe, A., Tensen, C. P., Smit, M. J., De Esch, I. J. & Leurs, R., 2005, In : Bioorganic and Medicinal Chemistry Letters. 15, 11, p. 2910-3Research output: Contribution to Journal › Article › Academic › peer-review
CXCR3 Receptors
Chemokine Receptors
Structure-Activity Relationship
Derivatives
Chemokines
The histamine H3 receptor: from gene cloning to H3 receptor drugs
Leurs, R., Bakker, R. A., Timmerman, H. & de Esch, I. J. P., 2005, In : Nature Reviews Drug Discovery. 4, 2, p. 107-20Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H3 Receptors
Histamine
Organism Cloning
Pharmaceutical Preparations
Genes
2004
8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist
Bakker, R. A., Weiner, D. M., ter Laak, T. L., Beuming, T., Zuiderveld, O. P., Edelbroek, M., Hacksell, U., Timmerman, H., Brann, M. R. & Leurs, R., 2004, In : Molecular Pharmacology. 65, 3, p. 538-49Research output: Contribution to Journal › Article › Academic › peer-review
Lisuride
Histamine Agonists
Histamine
8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist (vol 65, pg 538, 2004)
Bakker, R. A., Weiner, D. M., ter Laak, T. L., Beuming, T., Zuiderveld, O. P., Edelbroek, M., Hacksell, U., Timmerman, H., Brann, M. R. & Leurs, R., 2004, In : Molecular Pharmacology. 65, 4, p. 1048-1048Research output: Contribution to Journal › Article › Academic › peer-review
Lisuride
Histamine Agonists
Histamine
Activation of brain stem nuclei by improgan, a non-opioid analgesic
Nalwalk, J. B., Svokos, K., Taraschenko, O., Leurs, R., Timmerman, H. & Hough, L. H., 2004, In : Brain Research. 1021, 2, p. 248-55Research output: Contribution to Journal › Article › Academic › peer-review
Brain Stem
Analgesics
Periaqueductal Gray
Microinjections
Muscimol
Computational drug design: Method development and application to HIV inhibitor design
Vinkers, H. M., 2004Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
Open Access
File
Development and application to HIV inhibitor design
Vinkers, H. M., 2004Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
Differential activation of murine herpesvirus 68- and Kaposi's sarcoma-associated herpesvirus-encoded ORF74 G protein-coupled receptors by human and murine chemokines
Verzijl, D., Fitzsimons, C. P., Van Dijk, M., Stewart, J. P., Timmerman, H., Smit, M. J. & Leurs, R., 2004, In : Journal of Virology. 78, 7, p. 3343-51Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
File
Murid herpesvirus 4
Rhadinovirus
Human herpesvirus 8
Human Herpesvirus 8
chemokines
Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague-Dawley rats
Huang, Y. W., Hu, W., Chen, Z., Zhang, L. L., Shen, H. Q., Timmerman, H., Leurs, R. & Yanai, K., 2004, In : Behavioural Brain Research. 151, 1-2, p. 287-93Research output: Contribution to Journal › Article › Academic › peer-review
Fluorescent ligands for the histamine H2 receptor: synthesis and preliminary characterization
Malan, S. F., van Marle, A., Menge, W. M. P. B., Zuliana, V., Hoffman, M., Timmerman, H. & Leurs, R., 2004, In : Bioorganic and Medicinal Chemistry. 12, 24, p. 6495-503Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H2 Receptors
Ligands
Derivatives
Improgan-like analgesics: A family of compounds derived from histamine antagonists
Hough, L. H., Nalwalk, J. B., Menge, W. M. P. B., Leurs, R. & Timmerman, H., 2004, In : Medicinal Chemistry Research. 13, 1-2, p. 78-87Research output: Contribution to Journal › Article › Academic › peer-review
Histamine Antagonists
Analgesics
SKF 92374
Mutational analysis of the histamine H1-receptor binding pocket of histaprodifens
Bruysters, MWP., Pertz, H. H., Teunissen, A. W. R. H., Bakker, R. A., Gillard, M. R., Chatelain, P., Schunack, W., Timmerman, H. & Leurs, R., 2004, In : European Journal of Pharmacology. 487, 1-3, p. 55-63Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H1 Receptors
Histamine
histaprodifen
Pain-relieving drugs and the brain histaminergic system: multiple analgesic mechanisms from histamine, improgan and cimetidine
Hough, L. H., Nalwalk, J. B., Svokos, K., Leurs, R. & Timmerman, H., 2004, In : Inflammation Research. 53, p. S43-S44Research output: Contribution to Journal › Article › Academic › peer-review
2003
Effects of clobenpropit on pentylenetetrazole-kindled seizures in rats
Zhang, L. L., Chen, Z., Ren, K., Leurs, R., Chen, J. Y., Zhang, W., Ye, B., Wei, E. H. & Timmerman, H., 2003, In : European Journal of Pharmacology. 482, 1-3, p. 169-75Research output: Contribution to Journal › Article › Academic › peer-review
Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor
Casarosa, P., Menge, W. M. P. B., Minisini, R., Otto, C., van Heteren, J. T., Jongejan, A., Timmerman, H., Moepps, B., Kirchhoff, F., Mertens, T., Smit, M. J. & Leurs, R., 2003, In : Journal of Biological Chemistry. 278, 7, p. 5172-8Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
File
Improgan antinociception does not require neuronal histamine or histamine receptors
Izadi Mobarakeh, J., Nalwalk, J. B., Watanabe, T., Sakurada, S., Hoffman, M., Leurs, R., Timmerman, H., Silos-Santiago, I., Yanai, K. & Hough, L. H., 2003, In : Brain Research. 974, 1-2, p. 146-52Research output: Contribution to Journal › Article › Academic › peer-review
Histamine Receptors
Histamine
SKF 92374
Solid-phase synthesis of heterocyclic aromates: applicability towards combinatorial Chemistry: a review
Gelens, E., Menge, W. M. P. B., Koot, W. J., Ottenheijm, H. C. J. & Timmerman, H., 2003, In : Combinatorial Chemistry and High Throughput Screening. 6, p. 79-99 2 p.Research output: Contribution to Journal › Article › Academic › peer-review
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists
Govoni, M., Bakker, R. A., van de Wetering, I., Smit, M. J., Menge, W. M. P. B., Timmerman, H., Elz, S., Schunack, W. & Leurs, R., 2003, In : Journal of Medicinal Chemistry. 46, 26, p. 5812-24Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H1 Antagonists
Histamine Antagonists
Pharmacology
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists
Kitbunnadaj, R., Zuiderveld, O. P., De Esch, I. J., Vollinga, R. C., Bakker, R. A., Lutz, M., Spek, A. L., Cavoy, E., Deltent, M. F., Menge, W. M. P. B., Timmerman, H. & Leurs, R., 2003, In : Journal of Medicinal Chemistry. 46, 25, p. 5445-57Research output: Contribution to Journal › Article › Academic › peer-review
Structure-Activity Relationship
Human Activities
Histamine
4-(1H-imidazol-4-ylmethyl)piperidine
4-(1H-imidazol-4-yl)butanamine
The Solid-phase synthesis of substituted imidazoles via a scaffold approach
Gelens, E., 2003, 192 p.Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
2002
A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors
Booth, R. G., Moniri, N. H., Bakker, R. A., Choksi, N. Y., Nix, W. B., Timmerman, H. & Leurs, R., 2002, In : The Journal of Pharmacology and Experimental Therapeutics. 302, 1, p. 328-36Research output: Contribution to Journal › Article › Academic › peer-review
Histamine
tetralin
Histamine receptors: specific ligands, receptor biochemistry, and signal transduction
Bakker, R. A., Timmerman, H. & Leurs, R., 2002, In : Clinical Allergy and Immunology. 17, p. 27-64Research output: Contribution to Journal › Article › Academic › peer-review
Inhibition of improgan antinociception by the cannabinoid (CB)(1) antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-p yrazole-3-carboxamide (SR141716A): lack of obligatory role for endocannabinoids acting at CB(1) receptors
Hough, L. H., Nalwalk, J. B., Stadel, R., Timmerman, H., Leurs, R., Paria, B. C., Wang, X. W. & Dey, S. K., 2002, In : The Journal of Pharmacology and Experimental Therapeutics. 303, 1, p. 314-22Research output: Contribution to Journal › Article › Academic › peer-review
rimonabant
Cannabinoid Receptor Antagonists
Cannabinoid Receptors
Endocannabinoids
Cannabinoids
Kaposi's sarcoma-associated herpesvirus-encoded G protein-coupled receptor ORF74 constitutively activates p44/p42 MAPK and Akt via G(i) and phospholipase C-dependent signaling pathways
Smit, M. J., Verzijl, D., Casarosa, P., Navis, M., Timmerman, H. & Leurs, R., 2002, In : Journal of Virology. 76, 4, p. 1744-52Research output: Contribution to Journal › Article › Academic › peer-review
Open Access
File
Human herpesvirus 8
Human Herpesvirus 8
phospholipase C
Mitogen-Activated Protein Kinase 1
Type C Phospholipases
Methods to determine the constitutive activity of histamine H2 receptors
Leurs, R., Hoffmann, M., Alewijnse, A. E., Smit, M. J. & Timmerman, H., 2002, In : Methods in Enzymology. 343, p. 405-16Research output: Contribution to Journal › Article › Academic › peer-review
Role of histamine H3 receptors in control of mouse intestinal motility in vivo and in vitro: comparison with alpha2-adrenoceptors
Pozzoli, C., Todorov, S., Schunack, W., Timmerman, H., Coruzzi, G. & Poli, E., 2002, In : Digestive Diseases and Sciences. 47, p. 1065-72Research output: Contribution to Journal › Article › Academic › peer-review
Histamine H3 Receptors
Gastrointestinal Motility
Adrenergic Receptors
Histamine
Pharmaceutical Preparations
2001
antagonists for the human adenosine A3 receptor
van Muijlwijk-Koezen, J. E., 2001Research output: PhD Thesis › PhD Thesis - Research VU, graduation VU › Academic
A role for spinal, but not supraspinal, alpha(2) adrenergic receptors in the actions of improgan, a powerful, non-opioid analgesic
Svokos, K., Nalwalk, J. B., Leurs, R., Menge, W. M. P. B., Timmerman, H. & Hough, L. H., 2001, In : Brain Research. 923, 1-2, p. 12-9Research output: Contribution to Journal › Article › Academic › peer-review
Adrenergic alpha-2 Receptors
Cimetidine
Analgesics
SKF 92374