-Bicuculline-chemical-structure.gif)
(+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl- conductance generated by 40 μM GABA. (+)-Bicuculline inhibits GABA(A) α2/β1/γ2 currents activated by γ-Aminobutyric acid, (+)-Bicuculline concentration from 10 nM to 2 μM progressively decreased the amplitude of GABA-activated ion currents. Furthermore, (+)-bicuculine also blocks small-conductance calcium-activated potassium channels.
Eur J Pharmacol. 2022 Apr 5;920:174806.
Dexmedetomidine attenuates motor deficits via restoring the function of neurons in the nigrostriatal circuit in Parkinson's disease model mice
(+)-Bicuculline purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | Primary cortical neurons from rat E18 embryos |
| Preparation method | Bicuculline treatment could potentiate synaptic NMDAR signaling in the primary cortical neurons. Bicuculline led to a rapid decrease in STEP61 expression and a concomitant increase in the tyrosine phosphorylation of STEP substrates including GluN2B, Pyk2, and ERK1/2. |
| Concentrations | 10 μM |
| Incubation time | 15-60 min |
| Animal Experiment | |
|---|---|
| Animal models | Fischer-344 virgin female rats of Ovariectomy |
| Formulation | sesame oil + 10% DMSO |
| Dosages | 3.5 mg/kg daily |
| Administration | via osmotic subcutaneous pumps |
| Molecular Weight | 367.35 |
| Formula | C20H17NO6 |
| CAS Number | 485-49-4 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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