Sentence examples for binds at the convulsant from inspiring English sources
Here, we present evidence that RDX binds at the convulsant site of the γ-aminobutyric acid type A (GABAA) receptor (Benarroch 2007; Johnston 2005; Kalueff 2007), causing reduction of GABAA receptor mediated synaptic transmission and induction of epileptiform activity, as we demonstrate in the amygdala, a seizure-prone structure of the limbic system (Aroniadou-Anderjaska et al. 2007, 2008).
The potency of RDX at the GABAA convulsant site (Ki of 21.1 μM) is similar to pentylenetetrazol, a convulsant commonly used in animal models of seizure and epilepsy that is also known to bind at the picrotoxin convulsant site (Coulter et al. 1990).
Having found that RDX binds to the convulsant site of the GABAA receptor, we next examined the functional consequences by determining the effect of RDX on GABAA receptor– mediated currents in the basolateral nucleus of the amygdala (BLA).
The "cage convulsants," compounds with cyclical structure, bind at a convulsant binding pocket inside the GABAA ionophore at different and possibly overlapping positions.
The major finding of the present study is that RDX binds to the picrotoxin convulsant site of the GABAA receptor and inhibits GABAA receptor mediated synaptic transmission; this is likely to be the primary mechanism by which RDX induces brain seizures.
RDX displaced TBPS, a noncompetitive (for GABA) ionophore blocker, which acts at the picrotoxin convulsant site (Ito and Ho 1994; Kalueff 2007; Maksay and van Rijn 1993).
Epileptiform activity was induced in area CA3 of hippocampal slices by superfusion of medium containing 50 microM bicuculline and 3.5 mM K, 50 microM bicuculline and 5 mM K, 50 nM kainic acid and 3.5 mM K, or 7 mM K. Burst potentials were recorded at rates between 5 and 44/min, depending on the convulsant treatment.
