A pharmacological characterization of the mGluR1α subtype of the metabotropic glutamate receptor expressed in a cloned baby hamster kidney cell line

@article{Thomsen1993APC,
  title={A pharmacological characterization of the mGluR1$\alpha$ subtype of the metabotropic glutamate receptor expressed in a cloned baby hamster kidney cell line},
  author={Christian Thomsen and Eileen R. Mulvihill and Betty Haldeman and Darryl S. Pickering and David R. Hampson and Peter D. Suzdak},
  journal={Brain Research},
  year={1993},
  volume={619},
  pages={22-28}
}
CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.
TLDR
It is proposed that the interaction of CPCCOEt with Thr815 and Ala818 of mGluR1 disrupts receptor activation by inhibiting an intramolecular interaction between the agonist-bound extracellular domain and the transmembrane domain.
Enhanced type 1alpha metabotropic glutamate receptor-stimulated phosphoinositide signaling after pertussis toxin treatment.
TLDR
Changing changes in the concentration-effect curves for mGluR agonists are consistent with a model in which the receptor associates with PTX-sensitive inhibitory (Gi/o) and PTx-insensitive stimulatory (Gq/11) G proteins that can each influence PIC activity.
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