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  1. Article ; Online: M

    Dwomoh, Louis / Rossi, Mario / Scarpa, Miriam / Khajehali, Elham / Molloy, Colin / Herzyk, Pawel / Mistry, Shailesh N / Bottrill, Andrew R / Sexton, Patrick M / Christopoulos, Arthur / Conn, Jeffrey / Lindsley, Craig W / Bradley, Sophie J / Tobin, Andrew B

    Science signaling

    2022  Volume 15, Issue 760, Page(s) eabm3720

    Abstract: Many dementias are propagated through the spread of "prion-like" misfolded proteins. This includes prion diseases themselves (such as Creutzfeldt-Jakob disease) and Alzheimer's disease (AD), for which no treatments are available to slow or stop ... ...

    Abstract Many dementias are propagated through the spread of "prion-like" misfolded proteins. This includes prion diseases themselves (such as Creutzfeldt-Jakob disease) and Alzheimer's disease (AD), for which no treatments are available to slow or stop progression. The M
    MeSH term(s) Humans ; Animals ; Mice ; Prions/genetics ; Neurodegenerative Diseases/genetics ; Pathology, Molecular ; Proteomics ; Prion Diseases/genetics ; Alzheimer Disease/genetics ; Alzheimer Disease/pathology ; Receptor, Muscarinic M1/genetics ; Receptor, Muscarinic M1/metabolism
    Chemical Substances Prions ; Receptor, Muscarinic M1
    Language English
    Publishing date 2022-11-15
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2417226-1
    ISSN 1937-9145 ; 1945-0877
    ISSN (online) 1937-9145
    ISSN 1945-0877
    DOI 10.1126/scisignal.abm3720
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Modulation of the basal ganglia by metabotropic glutamate receptors: potential for novel therapeutics.

    Marino, Michael J / Conn, P Jeffrey / Conn, Jeffrey P

    Current drug targets. CNS and neurological disorders

    2003  Volume 1, Issue 3, Page(s) 239–250

    Abstract: The basal ganglia are implicated in a number of disorders including neurodegenerative motor diseases such as Huntington's and Parkinson's disease, as well as psychiatric disorders such as schizophrenia and obsessive compulsive disorder. In recent years, ... ...

    Abstract The basal ganglia are implicated in a number of disorders including neurodegenerative motor diseases such as Huntington's and Parkinson's disease, as well as psychiatric disorders such as schizophrenia and obsessive compulsive disorder. In recent years, a great deal of effort has been focused on determining the basal ganglia circuitry that underlies normal behavior, as well as many of these syndromes. This has led to a detailed understanding of both the normal and pathophysiological flow of information through the basal ganglia, and has provided the opportunity to begin developing novel pharmacological methods of intervention by targeting neuromodulatory receptors with in the basal ganglia circuit. One group of receptors that holds much promise for several basal ganglia disorders is the metabotropic glutamate receptors. Data from behavioral, neurochemical, neuroanatomical and electrophysiological studies has begun to reveal the functional roles that the metabotropic glutamate receptors play in modulating the basal ganglia circuit, and suggests that compounds selectively targeting these receptors may provide novel therapies for a variety of disorders including Parkinson's disease, addiction, and epilepsy.
    MeSH term(s) Animals ; Basal Ganglia/drug effects ; Basal Ganglia/metabolism ; Drug Delivery Systems/methods ; Humans ; Mental Disorders/drug therapy ; Mental Disorders/metabolism ; Receptors, Metabotropic Glutamate/metabolism
    Chemical Substances Receptors, Metabotropic Glutamate
    Language English
    Publishing date 2003-04-24
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 2146136-3
    ISSN 1568-007X
    ISSN 1568-007X
    DOI 10.2174/1568007023339319
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

    Alagille, David / DaCosta, Herve / Chen, Yelin / Hemstapat, Kamondanai / Rodriguez, Alice / Baldwin, Ronald M / Conn, Jeffrey P / Tamagnan, Gilles D

    Bioorganic & medicinal chemistry letters. 2011 June 1, v. 21, no. 11

    2011  

    Abstract: We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a–j,), (6-methylpyridin-2-yl)ethynyl (2a–j), (5-methylpyridin-2-yl)ethynyl (3a–j,), and ( ... ...

    Abstract We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a–j,), (6-methylpyridin-2-yl)ethynyl (2a–j), (5-methylpyridin-2-yl)ethynyl (3a–j,), and (pyridin-2-yl)ethynyl (4a–j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
    Keywords antagonists ; calcium ; glutamic acid ; in vitro studies ; receptors
    Language English
    Dates of publication 2011-0601
    Size p. 3243-3247.
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2011.04.047
    Database NAL-Catalogue (AGRICOLA)

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  4. Article ; Online: MGluR5 mediates the interaction between late-LTP, network activity, and learning.

    Bikbaev, Arthur / Neyman, Sergey / Ngomba, Richard Teke / Conn, P Jeffrey / Conn, Jeffrey / Nicoletti, Ferdinando / Manahan-Vaughan, Denise

    PloS one

    2008  Volume 3, Issue 5, Page(s) e2155

    Abstract: Hippocampal synaptic plasticity and learning are strongly regulated by metabotropic glutamate receptors (mGluRs) and particularly by mGluR5. Here, we investigated the mechanisms underlying mGluR5-modulation of these phenomena. Prolonged pharmacological ... ...

    Abstract Hippocampal synaptic plasticity and learning are strongly regulated by metabotropic glutamate receptors (mGluRs) and particularly by mGluR5. Here, we investigated the mechanisms underlying mGluR5-modulation of these phenomena. Prolonged pharmacological blockade of mGluR5 with MPEP produced a profound impairment of spatial memory. Effects were associated with 1) a reduction of mGluR1a-expression in the dentate gyrus; 2) impaired dentate gyrus LTP; 3) enhanced CA1-LTP and 4) suppressed theta (5-10 Hz) and gamma (30-100 Hz) oscillations in the dentate gyrus. Allosteric potentiation of mGluR1 after mGluR5 blockade significantly ameliorated dentate gyrus LTP, as well as suppression of gamma oscillatory activity. CA3-lesioning prevented MPEP effects on CA1-LTP, suggesting that plasticity levels in CA1 are driven by mGluR5-dependent synaptic and network activity in the dentate gyrus. These data support the hypothesis that prolonged mGluR5-inactivation causes altered hippocampal LTP levels and network activity, which is mediated in part by impaired mGluR1-expression in the dentate gyrus. The consequence is impairment of long-term learning.
    MeSH term(s) Allosteric Regulation ; Animals ; Dentate Gyrus/drug effects ; Dentate Gyrus/physiology ; Excitatory Amino Acid Antagonists/pharmacology ; Learning ; Long-Term Potentiation ; Male ; Memory ; Pyridines/pharmacology ; Rats ; Rats, Wistar ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate/antagonists & inhibitors ; Receptors, Metabotropic Glutamate/physiology
    Chemical Substances Excitatory Amino Acid Antagonists ; Grm5 protein, rat ; Pyridines ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate ; 6-methyl-2-(phenylethynyl)pyridine (7VC0YVI27Y)
    Language English
    Publishing date 2008-05-14
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1932-6203
    ISSN (online) 1932-6203
    DOI 10.1371/journal.pone.0002155
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.

    Alagille, David / DaCosta, Herve / Chen, Yelin / Hemstapat, Kamondanai / Rodriguez, Alice / Baldwin, Ronald M / Conn, P Jeffrey / Conn, Jeffrey P / Tamagnan, Gilles D

    Bioorganic & medicinal chemistry letters

    2011  Volume 21, Issue 11, Page(s) 3243–3247

    Abstract: We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and ( ... ...

    Abstract We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
    MeSH term(s) Acetylene/analogs & derivatives ; Acetylene/chemistry ; Acetylene/pharmacology ; Animals ; Binding, Competitive/drug effects ; Cells, Cultured ; Ligands ; Mice ; Molecular Structure ; Pyridines/chemistry ; Pyridines/pharmacology ; Rats ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate/antagonists & inhibitors ; Structure-Activity Relationship ; Thiazoles/chemistry ; Thiazoles/pharmacology
    Chemical Substances Grm5 protein, mouse ; Grm5 protein, rat ; Ligands ; Pyridines ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate ; Thiazoles ; phenylacetylene (239WSR2IBO) ; Acetylene (OC7TV75O83)
    Language English
    Publishing date 2011-04-20
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2011.04.047
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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  6. Article: Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity.

    Williams, Jacinta B / Mallorga, Pierre J / Lemaire, Wei / Williams, David L / Na, Sang / Patel, Smita / Conn, P Jeffrey / Conn, Jeffrey P / Pettibone, Douglas J / Austin, Christopher / Sur, Cyrille

    Analytical biochemistry

    2003  Volume 321, Issue 1, Page(s) 31–37

    Abstract: Human placental choriocarcinoma (JAR) cells endogenously expressing glycine transporter type 1a (GlyT1a) have been cultured in 96-well scintillating microplates to develop a homogenous screening assay for the detection of GlyT1 antagonists. In these ... ...

    Abstract Human placental choriocarcinoma (JAR) cells endogenously expressing glycine transporter type 1a (GlyT1a) have been cultured in 96-well scintillating microplates to develop a homogenous screening assay for the detection of GlyT1 antagonists. In these microplates uptake of [14C]glycine was time dependent and saturable with a Michaelis-Menten constant (Km) of 27+/-3 microM. The GlyT1 transport inhibitors sarcosine, ALX-5407, and Org-24598 were tested and shown to block [14C]glycine uptake with expected IC50 values of 37.5+/-4.6 microM, 2.8+/-0.6 nM, and 6.9+/-0.9 nM, respectively. The [14C]glycine uptake process was sensitive to membrane Na+ gradient as blockade of membrane Na+/K+-ATPase by ouabain or Na+ exchanger by benzamil-disrupted glycine accumulation in JAR cells. Glycine influx was not affected by concentration of dimethyl sulfoxide up to 2%. The versatility of this technological approach was further confirmed by the characterization of a saturable [14C]taurine uptake in JAR cells. Taurine transport was of high affinity with a Km of 10.2+/-1.7 microM and fully inhibited by ALX-5407 (IC50=522 +/-83 nM). The developed assay is homogenous, rapid, versatile and amenable to automation for the discovery of new neurotransmitter transporter inhibitors.
    MeSH term(s) Amino Acid Transport Systems, Neutral/genetics ; Amino Acid Transport Systems, Neutral/metabolism ; Carbon Radioisotopes ; Cell Count ; Cell Line, Tumor ; Chlorides/pharmacology ; Dose-Response Relationship, Drug ; Female ; Gene Expression Regulation, Neoplastic ; Glycine/antagonists & inhibitors ; Glycine/metabolism ; Glycine/pharmacology ; Glycine Plasma Membrane Transport Proteins ; Humans ; Pregnancy ; Scintillation Counting/methods ; Sodium/pharmacology ; Taurine/metabolism ; Time Factors
    Chemical Substances Amino Acid Transport Systems, Neutral ; Carbon Radioisotopes ; Chlorides ; Glycine Plasma Membrane Transport Proteins ; SLC6A9 protein, human ; Taurine (1EQV5MLY3D) ; Sodium (9NEZ333N27) ; Glycine (TE7660XO1C)
    Language English
    Publishing date 2003-04-21
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1110-1
    ISSN 1096-0309 ; 0003-2697
    ISSN (online) 1096-0309
    ISSN 0003-2697
    DOI 10.1016/s0003-2697(03)00431-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 389: Show issues Location:
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  7. Article: Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

    Alagille, David / DaCosta, Herve / Chen, Yelin / Hemstapat, Kamondanai / Rodriguez, Alice / Baldwin, Ronald M. / Conn, Jeffrey P. / Tamagnan, Gilles D.

    Bioorganic & medicinal chemistry letters

    Volume v. 21,, Issue no. 1

    Abstract: We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a–j,), (6-methylpyridin-2-yl)ethynyl (2a–j), (5-methylpyridin-2-yl)ethynyl (3a–j,), and ( ... ...

    Abstract We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a–j,), (6-methylpyridin-2-yl)ethynyl (2a–j), (5-methylpyridin-2-yl)ethynyl (3a–j,), and (pyridin-2-yl)ethynyl (4a–j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
    Keywords calcium ; in vitro studies ; glutamic acid ; receptors ; antagonists
    Language English
    Document type Article
    ISSN 0960-894X
    Database AGRIS - International Information System for the Agricultural Sciences and Technology

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