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  • binds
  • 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)
  • currents
  • 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)
  • We showed that the amino acid residues β2(Y157) and β3(Q185) mediate the positive modulatory effect of histamine on GABA-induced currents, whereas α1(R120) and β2(D163) form a potential histamine interaction site in GABA A Rs. (frontiersin.org)
  • affinity
  • γ2Phe77 was required for high affinity binding of the benzodiazepine site ligands flumazenil, CL218,872, and methyl-β-carboline-3-carboxylate but not flunitrazepam. (aspetjournals.org)
  • 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)
  • These data show that γ2Phe77 and γ2Met130 are necessary for high affinity binding of a number of benzodiazepine site ligands. (aspetjournals.org)
  • modulatory
  • In our study, we aimed to identify amino acids potentially involved in the modulatory effect of histamine on GABA A Rs. (frontiersin.org)
  • 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)
  • activate
  • Volatile agents such as desflurane may activate GABA channels and hyperpolarize cell membranes. (drugbank.ca)
  • site
  • The term "GABAc receptor" was first used by Johnston to describe a novel GABA binding site on neuronal membranes (Johnston, 1986, 1996). (utah.edu)
  • 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)
  • activity
  • This effect appears to be mediated in part by GABA A -R as increasing PKA activity also increased the duration of muscimol-induced LORR. (frontiersin.org)
  • Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking. (drugbank.ca)
  • cell
  • An example of a solitary rod-driven horizontal cell isolated from white perch retina is shown in Fig. 1, together with a typical GABA-elicited response from such a cell. (utah.edu)
  • shown
  • As shown in Fig. 1, GABA elicits a slow and sustained response from these cells. (utah.edu)
  • treat
  • Alprazolam, a benzodiazepine, is used to treat panic disorder and anxiety disorder. (drugbank.ca)
  • Lorazepam, a benzodiazepine not transformed to active metabolites, is used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia. (drugbank.ca)
  • Binding
  • 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)
  • In this hypothesis, steroid binding modifies GABA binding or signal transduction within the same β-α pair. (aspetjournals.org)
  • The term "GABAc receptor" was first used by Johnston to describe a novel GABA binding site on neuronal membranes (Johnston, 1986, 1996). (utah.edu)