Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.

@article{Lundstrm2011StructuralDO,
  title={Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators.},
  author={Linda Lundstr{\"o}m and Catarina Bissantz and Jennifer Wibbenmeyer Beck and Joseph G. Wettstein and Thomas Johannes Woltering and Juergen Wichmann and Silvia Gatti},
  journal={British journal of pharmacology},
  year={2011},
  volume={164 2b},
  pages={
          521-37
        }
}
BACKGROUND AND PURPOSE Altered glutamatergic neurotransmission is linked to several neurological and psychiatric disorders. Metabotropic glutamate receptor 2 (mGlu₂) plays an important role on the presynaptic control of glutamate release and negative allosteric modulators (NAMs) acting on mGlu₂/₃ receptors are under assessment for their potential as antidepressants, neurogenics and cognitive enhancers. Two new potent mGlu₂/₃ NAMs, RO4988546 and RO5488608, are described in this study and the… CONTINUE READING
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