Effect of cis- and trans-3-ACPBPA at GABA receptors expressed in X. laevis oocytes The IC50 values of cis- and trans-3-ACPBPA on GABACρ1 and ρ2 receptors expressed in X. laevis oocytes using the concentration of GABA as 1 μM are shown. The values in parentheses are log IC50 ± S.E.M.
Compound | GABAA(α1β2γ2L)a | GABAB(1b,2)b | IC50 | |||
|---|---|---|---|---|---|---|
| GABACρ1c | GABACρ2c | |||||
| % | μM | |||||
| cis-3-ACPBPA | 33 ± 3 | 27 ± 3 | 5.062 (0.7043 ± 0.025) | 11.08 (1.044 ± 0.086) | ||
| trans-3-ACPBPA | 28 ± 5 | 35 ± 5 | 72.58 (1.861 ± 0.043) | 189.7 (2.278 ± 0.034) | ||
↵ a Percentage inhibition cis-3-ACPBPA (1 mM) and trans-3-ACPBPA (1 mM) against an EC50 concentration of GABA (60 μM) at α1β2γ2L expressed in X. laevis oocytes
↵ b Percentage inhibition cis-3-ACPBPA (1 mM) and trans-3-ACPBPA (1 mM) against an EC50 concentration of GABA (3 μM) at GABAB(1b,2) coupled to GIRK1 and GIRK4 expressed in X. laevis oocytes