Henk Timmerman

em. prof. dr., prof. dr.

1985 …2014
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Research Output 1985 2014

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 JournalArticleAcademicpeer-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., 2010

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 39-44

Research output: Contribution to JournalArticleAcademicpeer-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 othersTimmerman, H., Talaga, P., Leurs, R. & Provins, L., 2009, In : ChemMedChem. 4, 7, p. 1063-8

Research output: Contribution to JournalArticleAcademicpeer-review

Medicinal chemistry teaching and training: a continuous adaptation

Timmerman, H. & de Souza, N. J., 2009, In : ChemMedChem. 4, 7, p. 1055-8

Research output: Contribution to JournalArticleAcademicpeer-review

Pharmaceutical Chemistry
Teaching

Obituary: To the Memory of Roelof Rekker

Timmerman, H. & Mannhold, R., 2009, In : QSAR and Combinatorial Science. 28, 5, p. 507-507

Research output: Contribution to JournalArticleAcademicpeer-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. 2944-53

Research output: Contribution to JournalArticleAcademicpeer-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. 94-103

Research output: Contribution to JournalArticleAcademicpeer-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. 172-9

Research output: Contribution to JournalArticleAcademicpeer-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. 53-87

Research output: Contribution to JournalArticleAcademicpeer-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. 281-91

Research output: Contribution to JournalArticleAcademicpeer-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. 117-23

Research output: Contribution to JournalArticleAcademicpeer-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. 2549-57

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Receptors
Histamine

Gamma-herpesvirus-encoded G-protein-coupled receptors

Verzijl, D., 2006

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 35327-35

Research output: Contribution to JournalArticleAcademicpeer-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. 1390-400

Research output: Contribution to JournalArticleAcademicpeer-review

Mutational analysis of the human histamine H1 receptor

Bruysters, MWP., 2006

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

2005

Isolation and structure elucidation of tracheospasmolytic compounds from piper cubeba l.f fruits and their possibility as anti-inslammatory activity

Wahyono, Z., 2005

Research output: PhD ThesisPhD Thesis - Research external, graduation externalAcademic

Isolation and structure elucidation of tracheospasmolytic compounds from vitex trifolia l. leaves

Alam, G., 2005

Research output: PhD ThesisPhD Thesis - Research external, graduation externalAcademic

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. 6309-23

Research output: Contribution to JournalArticleAcademicpeer-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. 2100-7

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine Agonists
Imidazoles
Histamine
methimepip

Synthesis and In Vitro Pharmacological Evaluation of Novel Ligands for Histamine Receptors

Govoni, M., 2005

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 2910-3

Research output: Contribution to JournalArticleAcademicpeer-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. 107-20

Research output: Contribution to JournalArticleAcademicpeer-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. 538-49

Research output: Contribution to JournalArticleAcademicpeer-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. 1048-1048

Research output: Contribution to JournalArticleAcademicpeer-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. 248-55

Research output: Contribution to JournalArticleAcademicpeer-review

Brain Stem
Analgesics
Periaqueductal Gray
Microinjections
Muscimol

Computational drug design: Method development and application to HIV inhibitor design

Vinkers, H. M., 2004

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

Open Access
File

Development and application to HIV inhibitor design

Vinkers, H. M., 2004

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 3343-51

Research output: Contribution to JournalArticleAcademicpeer-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. 287-93

Research output: Contribution to JournalArticleAcademicpeer-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. 6495-503

Research output: Contribution to JournalArticleAcademicpeer-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. 78-87

Research output: Contribution to JournalArticleAcademicpeer-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. 55-63

Research output: Contribution to JournalArticleAcademicpeer-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-S44

Research output: Contribution to JournalArticleAcademicpeer-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. 169-75

Research output: Contribution to JournalArticleAcademicpeer-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. 5172-8

Research output: Contribution to JournalArticleAcademicpeer-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. 146-52

Research output: Contribution to JournalArticleAcademicpeer-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 JournalArticleAcademicpeer-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. 5812-24

Research output: Contribution to JournalArticleAcademicpeer-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. 5445-57

Research output: Contribution to JournalArticleAcademicpeer-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 ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 328-36

Research output: Contribution to JournalArticleAcademicpeer-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. 27-64

Research output: Contribution to JournalArticleAcademicpeer-review

rimonabant
Cannabinoid Receptor Antagonists
Cannabinoid Receptors
Endocannabinoids
Cannabinoids
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. 405-16

Research output: Contribution to JournalArticleAcademicpeer-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. 1065-72

Research output: Contribution to JournalArticleAcademicpeer-review

Histamine H3 Receptors
Gastrointestinal Motility
Adrenergic Receptors
Histamine
Pharmaceutical Preparations
2001

antagonists for the human adenosine A3 receptor

van Muijlwijk-Koezen, J. E., 2001

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

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. 12-9

Research output: Contribution to JournalArticleAcademicpeer-review

Adrenergic alpha-2 Receptors
Cimetidine
Analgesics
SKF 92374