(A, B) Modulation of chloride currents through GABAA receptors composed of α1, β2,
and γ2S subunits by 100 μM piperine and the
indicated derivatives (dotted line indicates cutoff for highly active
compounds). (C, D) Concentration-dependent IGABA (EC3–7) enhancement through α1β2γ2S GABAA receptors:
(C) by 47 (■), 53 (▲), and 72 (●), ranked by efficiency, and (D) by 56 (▲) and 73 (●), ranked by potency, compared
to piperine (dotted line). (E, F) Representative IGABA modulated by (E) 72 and (F) 73. Data represent mean ± SEM from at least three oocytes and
two oocyte batches. Asterisks indicate statistically significant differences
from zero: *p < 0.05, **p <
0.01. Data for piperine were taken from ref (31).