Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors.

@article{Mhlemann2006DeterminationOK,
  title={Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors.},
  author={Andreas M{\"u}hlemann and Natalie A Ward and Nicole A. Kratochwil and Catherine Diener and Christophe Fischer and Andy Stucki and Georg Jaeschke and Pari Malherbe and Richard H. P. Porter},
  journal={European journal of pharmacology},
  year={2006},
  volume={529 1-3},
  pages={
          95-104
        }
}
Several mutations in the seven-transmembrane region of rat metabotropic glutamate 5 (rmGlu5) receptors were produced by site-directed mutagenesis and expressed in CHO cells. Using functional intracellular calcium ([Ca(2+)](i)) mobilisation, we identified amino acids implicated in the positive allosteric modulation of quisqualate-induced response by 3,3'-difluorobenzaldazine (DFB). Human and rat mGlu5 receptors displayed a higher potency and a higher efficacy in the presence of DFB. Mutant… CONTINUE READING
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