• About
    • Login
    View Item 
    •   Institutional Repository Home
    • Electronic Theses and Dissertations
    • Electronic Theses and Dissertations
    • View Item
    •   Institutional Repository Home
    • Electronic Theses and Dissertations
    • Electronic Theses and Dissertations
    • View Item
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Browse

    All of Institutional RepositoryCommunities & CollectionsBy Issue DateAuthorsTitlesSubjectsDepartmentThis CollectionBy Issue DateAuthorsTitlesSubjectsDepartment

    My Account

    LoginRegister

    Discovery, Optimization, and Characterization of Novel Subtype-Selective Muscarinic Acetylcholine Receptor M4 and M5 Positive Allosteric Modulators

    Bridges, Thomas Miller
    : https://etd.library.vanderbilt.edu/etd-09202010-221417
    http://hdl.handle.net/1803/14185
    : 2010-09-21

    Abstract

    There exist five subtypes of the muscarinic acetylcholine receptor (M1-M5), which are differentially expressed throughout the body and play important roles in numerous physiological processes, including autonomic functions, motor control, cognition, reward, and sleep, among others. A historic lack of small molecules possessing high subtype-selectivity has hampered basic neurobiological research into the roles of each subtype in the central nervous system and has precluded successful therapeutic development of muscarinic ligands targeting a particular receptor subtype. Functional cell-based screening in conjunction with medicinal chemistry techniques were performed in order to discover highly subtype-selective allosteric ligands for M1, M4, and M5. Multiple series of M1 positive allosteric modulators, M1 allosteric agonists, M1 antagonists, M4 positive allosteric modulators, and the first series of selective M5 positive allosteric modulators were successfully discovered, optimized, and characterized.
    Show full item record

    Files in this item

    Icon
    Name:
    Bridges.pdf
    Size:
    16.84Mb
    Format:
    PDF
    View/Open

    This item appears in the following collection(s):

    • Electronic Theses and Dissertations

    Connect with Vanderbilt Libraries

    Your Vanderbilt

    • Alumni
    • Current Students
    • Faculty & Staff
    • International Students
    • Media
    • Parents & Family
    • Prospective Students
    • Researchers
    • Sports Fans
    • Visitors & Neighbors

    Support the Jean and Alexander Heard Libraries

    Support the Library...Give Now

    Gifts to the Libraries support the learning and research needs of the entire Vanderbilt community. Learn more about giving to the Libraries.

    Become a Friend of the Libraries

    Quick Links

    • Hours
    • About
    • Employment
    • Staff Directory
    • Accessibility Services
    • Contact
    • Vanderbilt Home
    • Privacy Policy