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Fig 1. Consensus subunit arrangement of α1β2γ2 GABAA receptors and three newly proposed receptors with unconventional subunit arrangement.Number of predicted agonist sites for GABA and modulatory sites for benzodiazepines (BZ) is shown for each receptor form. On the top left is the color code for the subunits.
Fig 2. Dual and triple concatenated constructs used for the construction of pentameric receptors were expressed in Xenopus oocytes.Currents were standardized to the amplitude elicited in oocytes expressing non-concatenated α1, β2 and γ2 subunits (non-concatenated receptors). The same parameters are shown for receptors with consensus subunit arrangement (consensus receptors) that were built in three different ways and for three receptors with non-consensus subunit arrangement (non-consensus receptors), one of them built in two different ways. For some receptors, stimulation by 1 μM diazepam is also shown.
Fig 3. Concentration-response curves for β2-α1-γ2, β2-α1-γ2/α1-γ2 and β2-α1-γ2/β2-γ2 receptors.Receptors were exposed to subsequently higher concentrations of GABA and the elicited current amplitude was determined. Individual curves were first normalized to the fitted maximal current amplitude and subsequently averaged. Data are expressed as mean ± S.D., n = 3–5 from two batches of oocytes. A) Original current traces recorded in an oocyte expressing β2-α1-γ2/β2-γ2. B) Averaged Concentration-response curves for β2-α1-γ2, β2-α1-γ2/α1-γ2 and β2-α1-γ2/β2-γ2.
Fig 4. Stimulation of β2-α1-γ2, β2-α1-γ2/α1-γ2, β2-α1-γ2/β2-γ2 and α1/β2/γ2 receptors by diazepam.Receptors were exposed to subsequently higher concentrations of diazepam in combination with an EC2 GABA concentration and the elicited current amplitude was determined. Individual curves were first normalized to the fitted maximal current amplitude and subsequently averaged. Data are expressed as mean ± S.D., n = 3 from two batches of oocytes.
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