[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.

@article{Anderson20023HMethoxymethyl32methyl13thiazol4,
  title={[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.},
  author={Jeffrey John Anderson and Santosh Uttarkar Panduranga Rao and Blake Alan Rowe and Darlene R Giracello and Greg Holtz and Deborah F. Chapman and Lida R Tehrani and Margaret J. Bradbury and Nicholas D. P. Cosford and Mark Andrew Varney},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={303 3},
  pages={
          1044-51
        }
}
The binding of [3H]methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (methoxymethyl-MTEP), a potent and selective antagonist for metabotropic glutamate (mGlu)5 receptors, was characterized in rat brain both in vitro and in vivo. Nonspecific binding, as defined with 10 microM 2-methyl-6-(phenylethynyl)-pyridine (MPEP), was less than 10% of total binding in rat brain membranes. The binding of [3H]methoxymethyl-MTEP was of high affinity (K(d) = 20 +/- 2.7 nM), saturable (B(max) = 487… CONTINUE READING

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