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  1. Article ; Online: Probing Adenosine and P2 Receptors: Design of Novel Purines and Nonpurines as Selective Ligands.

    Jacobson, Kenneth A

    Drug development research

    2024  Volume 52, Issue 1-2, Page(s) 178–186

    Abstract: Recent approaches to the design of selective agonists and antagonists at adenosine (AR) and P2 receptors include both modifying known receptor ligands and searching for structurally diverse antagonists. The ribose-like moiety of nucleoside/nucleotide ... ...

    Abstract Recent approaches to the design of selective agonists and antagonists at adenosine (AR) and P2 receptors include both modifying known receptor ligands and searching for structurally diverse antagonists. The ribose-like moiety of nucleoside/nucleotide derivatives was rigidified with a methanocarba (mc) modification, to constrain the ring in a conformation that was favored in binding to ARs or P2Y receptors. (N)-mc analogs of various N
    Language English
    Publishing date 2024-01-18
    Publishing country United States
    Document type Journal Article
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/ddr.1113
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Book ; Online: Purinergic Pharmacology

    Ciruela, Francisco / Jacobson, Kenneth A.

    2019  

    Keywords Science: general issues ; Pharmacology ; Adenosine ; G protein-coupled purinergic receptors ; ATP ; purinergic signalling ; Adenosine transport ; Caffeine ; Purinergic pathophysiology ; Ligand-gated purinergic ion channels
    Size 1 electronic resource (852 pages)
    Publisher Frontiers Media SA
    Document type Book ; Online
    Note English ; Open Access
    HBZ-ID HT021231157
    ISBN 9782889459476 ; 2889459470
    Database ZB MED Catalogue: Medicine, Health, Nutrition, Environment, Agriculture

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  3. Article: Editorial: Purinergic pharmacology, Volume II.

    Ciruela, Francisco / Jacobson, Kenneth A

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1200187

    Language English
    Publishing date 2023-05-16
    Publishing country Switzerland
    Document type Editorial
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1200187
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Book: Pharmacology of purine and pyrimidine receptors

    Jacobson, Kenneth A. / Linden, Joel

    (Advances in pharmacology ; 61)

    2011  

    Author's details ed. by Kenneth A. Jacobson ; Joel Linden
    Series title Advances in pharmacology ; 61
    Collection
    Language English
    Size XVI, 541 S. : Ill., graph. Darst.
    Edition 1. ed.
    Publisher Elsevier Acad. Press
    Publishing place Amsterdam u.a.
    Publishing country Netherlands
    Document type Book
    HBZ-ID HT016920122
    ISBN 978-0-12-385526-8 ; 0-12-385526-8
    Database Catalogue ZB MED Medicine, Health

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  5. Article ; Online: Effects of Combinations of Methylxanthines and Adenosine Analogs on Locomotor Activity in Control and Chronic Caffeine-Treated Mice.

    Nikodijević, Olga / Jacobson, Kenneth A / Daly, John W

    Drug development research

    2024  Volume 30, Issue 2, Page(s) 104–110

    Abstract: Chronic caffeine ingestion (CCI) by male NIH Swiss strain mice results in a prolonged reduction in locomotor activity and alterations in response to caffeine, other xanthines, and adenosine analogs. Caffeine, the ... ...

    Abstract Chronic caffeine ingestion (CCI) by male NIH Swiss strain mice results in a prolonged reduction in locomotor activity and alterations in response to caffeine, other xanthines, and adenosine analogs. Caffeine, the A
    Language English
    Publishing date 2024-01-05
    Publishing country United States
    Document type Journal Article
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/ddr.430300209
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Editorial: Small molecules and biologics for future purinergic therapeutics.

    Jacobson, Kenneth A / Salvemini, Daniela

    Purinergic signalling

    2023  Volume 19, Issue 3, Page(s) 465–466

    Abstract: Receptor agonists and antagonists and other modulators of purinergic signalling have potential as novel therapeutics for a broad range of diseases and conditions. This special issue focuses on compounds or approaches that are either in clinical trials or ...

    Abstract Receptor agonists and antagonists and other modulators of purinergic signalling have potential as novel therapeutics for a broad range of diseases and conditions. This special issue focuses on compounds or approaches that are either in clinical trials or headed in that direction. It is intended to serve as an up-to-date description of selected efforts to discover and develop new small molecular purinergic drugs.
    MeSH term(s) Receptors, Purinergic P2X/metabolism ; Biological Products ; Signal Transduction
    Chemical Substances Receptors, Purinergic P2X ; Biological Products
    Language English
    Publishing date 2023-09-07
    Publishing country Netherlands
    Document type Editorial ; Research Support, N.I.H., Intramural ; Research Support, N.I.H., Extramural
    ZDB-ID 2172143-9
    ISSN 1573-9546 ; 1573-9538
    ISSN (online) 1573-9546
    ISSN 1573-9538
    DOI 10.1007/s11302-023-09964-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Optical Control of Adenosine A

    Ciruela, Francisco / Jacobson, Kenneth A

    Frontiers in immunology

    2022  Volume 13, Page(s) 904762

    MeSH term(s) Adenosine ; Humans ; Phototherapy ; Psoriasis/therapy ; Signal Transduction
    Chemical Substances Adenosine (K72T3FS567)
    Language English
    Publishing date 2022-04-29
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2606827-8
    ISSN 1664-3224 ; 1664-3224
    ISSN (online) 1664-3224
    ISSN 1664-3224
    DOI 10.3389/fimmu.2022.904762
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Tribute to Prof. Geoffrey Burnstock: transition of purinergicsignaling to drug discovery.

    Jacobson, Kenneth A

    Purinergic signalling

    2020  Volume 17, Issue 1, Page(s) 3–8

    Abstract: Geoffrey Burnstock made a chance observation early in his research career that did not fit the conventional scientific dogma-non-noradrenergic, non-cholinergic (NANC) nerves. Instead of rejecting these as an artifact, he followed their logical course to ... ...

    Abstract Geoffrey Burnstock made a chance observation early in his research career that did not fit the conventional scientific dogma-non-noradrenergic, non-cholinergic (NANC) nerves. Instead of rejecting these as an artifact, he followed their logical course to characterize the actions of extracellular ATP on nerves and muscles, eventually founding a large branch of pharmacology around purinergic signaling. The solid proof that validated his concept and dismissed many detractors was the cloning of seven ionotropic P2X receptors and eight metabotropic P2Y receptors, which are expressed in some combination in every tissue and organ. Given the broad importance of this signaling system in biology, medicinal chemists, inspired by Burnstock, began creating synthetic agonists and antagonists for these purinergic receptors. Various ligands have advanced to clinical trials, for disorders of the immune, nervous, cardiovascular, and other systems, and a few are already approved. Thus, medically important approaches have been derived from Burnstock's original pharmacological concepts and his constant guiding of the course of the field. The therapeutic potential of modulators of purinergic signaling is vast.
    MeSH term(s) Adenosine Triphosphate/metabolism ; Animals ; Drug Discovery ; Humans ; Receptors, Purinergic/metabolism ; Signal Transduction/physiology
    Chemical Substances Receptors, Purinergic ; Adenosine Triphosphate (8L70Q75FXE)
    Language English
    Publishing date 2020-08-14
    Publishing country Netherlands
    Document type Journal Article ; Research Support, N.I.H., Intramural ; Review
    ZDB-ID 2172143-9
    ISSN 1573-9546 ; 1573-9538
    ISSN (online) 1573-9546
    ISSN 1573-9538
    DOI 10.1007/s11302-020-09717-y
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: A

    Jacobson, Kenneth A / Suresh, R Rama / Oliva, Paola

    International review of neurobiology

    2023  Volume 170, Page(s) 1–27

    Abstract: The Gs-coupled ... ...

    Abstract The Gs-coupled A
    MeSH term(s) Humans ; Purinergic P1 Receptor Agonists ; Drug Inverse Agonism ; Alzheimer Disease ; Immunotherapy ; Neuroprotective Agents ; Parkinson Disease/drug therapy
    Chemical Substances Purinergic P1 Receptor Agonists ; Neuroprotective Agents
    Language English
    Publishing date 2023-08-25
    Publishing country United States
    Document type Journal Article
    ZDB-ID 209876-3
    ISSN 2162-5514 ; 0074-7742
    ISSN (online) 2162-5514
    ISSN 0074-7742
    DOI 10.1016/bs.irn.2023.08.001
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: 1,3-Dialkylxanthine Derivatives Having High Potency as Antagonists at Human A

    Jacobson, Kenneth A / IJzerman, Ad P / Linden, Joel

    Drug development research

    2023  Volume 47, Issue 1, Page(s) 45–53

    Abstract: The structure-activity relationships (SAR) of alkylxanthine derivatives as antagonists at the recombinant human adenosine receptors were explored in order to identify selective antagonists of ... ...

    Abstract The structure-activity relationships (SAR) of alkylxanthine derivatives as antagonists at the recombinant human adenosine receptors were explored in order to identify selective antagonists of A
    Language English
    Publishing date 2023-11-27
    Publishing country United States
    Document type Journal Article
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/(sici)1098-2299(199905)47:1<45::aid-ddr6>3.0.co;2-u
    Database MEDical Literature Analysis and Retrieval System OnLINE

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