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. 2019 Mar 6;149(1):41–53. doi: 10.1111/jnc.14646

Table 2.

Association (k on) and dissociation (k off) rate constants of [3H]muscimol binding at room temperature in forebrain and cerebellar membranes of WT and δKO mice and in recombinant receptors expressed in HEK293 cells

k on(M−1 × min−1) k off(min−1) K D(nM)
Forebrain membranes
WT mice 3.3 ± 0.2 × 108 0.53 ± 0.02 1.6
δKO mice 15 ± 3.1 × 108 ** 1.67 ± 0.15*** 1.1
WT‐δKO 1.4 ± 0.2 × 108 0.23 ± 0.02 1.6
Cerebellar membranes
 WT mice 2.8 ± 0.2 × 108 0.47 ± 0.14 1.7
 δKO mice 7.7 ± 0.2 × 108 ** 1.11 ± 0.09* 1.4
 WT‐δKO 1.2 ± 0.2 × 108 0.12 ± 0.03 1.0
Recombinant receptors
 α1β2 n.d. 0.49 ± 0.07###
 α1β2γ2 11 ± 0.6 × 108 1.78 ± 0.18 1.6
 α1β2δ n.d. 0.18 ± 0.03###
 α6β2 n.d. 1.46 ± 0.05†††
 α6β2γ2 6.3 ± 0.5 × 108, ### , ††† 0.98 ± 0.02### , ††† 1.6
 α6β2δ 1.0 ± 0.1 × 108, ### 0.13 ± 0.03### 1.3
 α6β3δ 1.8 ± 0.1 × 108, ### 0.13 ± 0.01### 0.72

Association (k on) and dissociation rate constants (k off) of [3H]muscimol binding in forebrain samples (association, n = 8, dissociation, n = 4 independent experiments made using individual animal forebrains) and in samples each of pooled from 3 mouse cerebella (n = 3 independent experiments made using pooled samples from 3 individual animal cerebella), and in recombinant receptors (n = 3–6 independent experiments each performed using receptors from independent transfections/expressions) (mean ± SEM). n.d., not determined. All experiments were performed in triplicate technical replicates. Statistical comparison of forebrain and cerebellar values: *p < 0.05, **p < 0.01, ***p < 0.001, significantly different from the corresponding WT value, unpaired t‐test. Statistical comparison of recombinant receptor values: ###p < 0.001, significantly different from the corresponding α1β2γ2 value; †††p < 0.001, significantly different from the corresponding α6β2δ value (one‐way anova followed by Tukey's post hoc test).