Agonistic effects of the β-carboline DMCM revealed in GABAA receptor γ2 subunit F77I point-mutated mice

@article{Lepp2005AgonisticEO,
  title={Agonistic effects of the $\beta$-carboline DMCM revealed in GABAA receptor $\gamma$2 subunit F77I point-mutated mice},
  author={E. Lepp{\"a} and O. Vekovischeva and A. Linden and P. Wulff and A. Oberto and W. Wisden and E. Korpi},
  journal={Neuropharmacology},
  year={2005},
  volume={48},
  pages={469-478}
}
Abstract Affinity of the inverse agonist methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) to the benzodiazepine binding site of the GABA A receptor is abolished by a phenylalanine (F) to isoleucine (I) substitution at position 77 of the γ2 subunit. We tested the effects of DMCM in gene knockin γ2I77 mice carrying this mutation. Unlike in wild-type mice, DMCM was not able to reverse the GABA-induced reduction of the picrotoxin-sensitive t -butylbicyclophosphoro-[ 35 S]thionate ([ 35… Expand
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