Bicuculline

Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABA_A receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice^[1][2][3][4]. IC50 & Target:IC50: 2 μM (GABA_A)^[3] In Vitro: Bicuculline (1 and 3 μM) attains the maximal response of GABA. Bicuculline appears to shift the dose-response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at α₁β₂γ_2L GABA_A receptors^[3]. In Vivo: Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Bicuculline can be used to induce seizure models. In Sprague-Dawley rats, the pharmacokinetic parameters of orally administered Bicuculline (15 mg/kg) include a half-life of 1.6 hours, an AUC_{(0 t)} of 109.0 ng/mL·h, a C_max of 40 ng/mL, and a clearance rate of 144.5 L/h/kg^[6].