Agonistic effects of the beta-carboline DMCM revealed in GABA(A) receptor gamma 2 subunit F77I point-mutated mice.

@article{Lepp2005AgonisticEO,
  title={Agonistic effects of the beta-carboline DMCM revealed in GABA(A) receptor gamma 2 subunit F77I point-mutated mice.},
  author={Elli Lepp{\"a} and Olga Vekovischeva and A M Lind{\'e}n and Peer Wulff and Alessandra Oberto and William Wisden and Esa R Korpi},
  journal={Neuropharmacology},
  year={2005},
  volume={48 4},
  pages={469-78}
}
Affinity of the inverse agonist methyl-6,7-dimethoxy-4-ethyl-beta-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 gamma2 subunit. We tested the effects of DMCM in gene knockin gamma2I77 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-[35S]thionate ([35S… CONTINUE READING

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