• affinity
  • In contrast, γ2Met130 was required for high affinity binding of flunitrazepam, clonazepam, and triazolam but not flumazenil, CL218,872, or methyl-β-carboline-3-carboxylate and did not affect benzodiazepine efficacy. (aspetjournals.org)
  • Introduction of the phenylalanine and methionine into the appropriate positions of γ1 was not sufficient to confer high affinity for the benzodiazepine site ligand zolpidem. (aspetjournals.org)
  • chloride
  • Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. (drugbank.ca)
  • affects
  • Here, we have investigated whether the sites for GABA and steroids are functionally linked (i.e., whether the occupancy of a steroid site selectively affects activation elicited by GABA binding to the transmitter binding site within the same β-α pair). (aspetjournals.org)
  • oocytes
  • We expressed GABA A Rs with 12 different point mutations in Xenopus laevis oocytes and characterized the effect of histamine on GABA-induced currents using the two-electrode voltage clamp technique. (frontiersin.org)
  • site
  • Furthermore, γ2Phe77 is homologous to α1Phe64, which has been previously shown to be a key determinant of the GABA binding site, suggesting a conservation of motifs between different ligand binding sites on the GABA A receptor. (aspetjournals.org)
  • We conclude that steroids potentiate the opening of the GABA A receptor induced by either agonist binding site. (aspetjournals.org)
  • major
  • The GABA A receptor, the major target of many exogenous neuroactive steroids, binds synaptically released or ambient GABA, resulting in the activation of an anion-selective channel. (aspetjournals.org)
  • Currently
  • With these criteria, we develop a working GABA A receptor list, which currently includes 26 members, but will undoubtedly be modified and grow as information expands. (aspetjournals.org)