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Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents
The discovery of a potent and selective small-molecule inhibitor of Wee1 kinase, MK-1775, and its data indicate that Wee1 inhibition provides a new approach for treatment of multiple human malignancies.
Pharmacological Effects of the Metabotropic Glutamate Receptor 1 Antagonist Compared with Those of the Metabotropic Glutamate Receptor 5 Antagonist and Metabotropic Glutamate Receptor 2/3 Agonist in…
- A. Satow, S. Maehara, H. Ohta
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 August 2008
Investigation of the functional roles of metabotropic glutamate receptor (mGluR) 1 in integrative brain functions showed antipsychotic-like effects without impairing motor functions, whereas blockade of mGLUR5 and activation of mgluR2/3 did not display such activities.
Pharmacological Characterization of a New, Orally Active and Potent Allosteric Metabotropic Glutamate Receptor 1 Antagonist,…
- G. Suzuki, Toshifumi Kimura, H. Ohta
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 June 2007
FTIDC is a highly potent and selective allosteric mGluR1 antagonist and a compound having oral activity without species differences in its antagonistic activity on recombinant human, mouse, and rat mGlamR1 and could be a valuable tool for elucidating the functions of mGLUR1 not only in rodents but also in humans.
Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor…
Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist,…
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
A potent M(3) antagonist, 14a (K(i) = 0.31 nM), with novel structural features was identified, which showed high selectivity for M( 3) receptors over the other muscarinic receptor subtypes.
Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.
Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists.
The relationship between receptor occupancy and in vivo pharmacological activity of mGluR1 antagonists was clarified and receptor occupancy assays could help provide guidelines for selecting appropriate doses of allosteric mGLUR1 antagonist for examining the function of mR1 in vivo.
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Calcium-dependent Conformation of a Mouse Macrophage Calcium-type Lectin
Results indicate that there is a positive cooperativity between the lectin's ligand binding site and its physically distinct calcium-dependent epitope, especially in a low calcium environment.