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Design and syntheses of caged mGluR6 antagonists for studies on dynamic signaling mechanisms in ON bipolar cells

Wednesday, October 26, 2011 — Poster Session III

10:00 a.m. – Noon

Natcher Conference Center




  • Z-D Shi
  • A Sulima
  • H Wu
  • W Kothmann
  • J Diamond
  • GL Griffiths


A metabotropic glutamate receptor, mGluR6, is a G protein-coupled receptor that is expressed only in ON bipolar cells in retina and is activated by the neurotransmitter, glutamate. Activation of mGluR6 results in hyperpolarized ON bipolar cells. Mechanisms of the intracellular signaling cascade are still poorly understood because the slow photoreceptor response to light makes it difficult to discern many important physiological characteristics of the synapses. ON bipolar cells can be depolarized using competitive mGluR6 antagonists. Based on these findings, we designed two caged (non-fluorescent) mGluR6 antagonists to enable consistent stimulation of ON bipolar cells at 1000 times faster speeds than photoreceptors. The first is the caged compound 1-(4,5-dimethoxy-2-nitrophenyl)ethyl-caged cyclopropyl-4-phosphonophenylglycine (DMNPE-caged CPPG) and the second is coumarin-caged alfa-methyl-3-methoxy-4-phosphonophenylglycine (coumarin-caged UBP1111). The detailed background, design and syntheses will be described.

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