8 research outputs found

    Design of 4‚ÄĎOxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

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    Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu<sub>2/3</sub> inhibition and a variety of CNS diseases and disorders. Though these tools typically have good selectivity for mGlu<sub>2/3</sub> versus the remaining six members of the mGlu family, compounds that are selective for only one of the individual group II mGlus have proved elusive. Herein we report on the discovery of a potent and highly selective mGlu<sub>2</sub> negative allosteric modulator <b>58</b> (VU6001192) from a series of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides. The concept for the design of this series centered on morphing a quinoline series recently disclosed in the patent literature into a chemotype previously used for the preparation of muscarinic acetylcholine receptor subtype 1 positive allosteric modulators. Compound <b>58</b> exhibits a favorable profile and will be a useful tool for understanding the biological implications of selective inhibition of mGlu<sub>2</sub> in the CNS

    Bourdon's arithmetic : containing a discussion of the theory of numbers /

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    Publisher's advertisements: [4] p. at end of vol.Mode of access: Internet

    SLAVERY: ANNUAL BIBLIOGRAPHICAL SUPPLEMENT (2005)

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    Notes on elements of (analytical) solid geometry /

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    Spine title: Venable's notes on solid geometry.Mode of access: Internet

    Synthesis and characterization of first row transition metal p-toluenesulfonate complexes and chains

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