Bicuculline

SKU: orb1304933

Description

Bicuculline is a natural alkaloid that acts as a competitive GABAA receptor antagonist (IC50 = 2 µM) and a blocker of SK potassium channels. It is widely utilized in neuroscience research to induce seizures in animal models and to study synaptic inhibition and neuronal excitability in vitro.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 485-49-4
• MW: 367.35
• Purity: 99.99% (May vary between batches)
• Formula: C₂₀H₁₇NO₆
• SMILES: [H][C@]1(OC(=O)c2c3OCOc3ccc12)[C@@]1([H])N(C)CCc2cc3OCOc3cc12
• Target: GABA Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.44 mM);DMSO:16.67 mg/mL (45.38 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  GABAA receptor:2 μM
• In Vivo:
  (+)-Bicuculline, at concentrations of 1/3 μM, increased the EC50 of gamma-aminobutyric acid (GABA) by 1.6 times (41.0-67.0 μM) and by 3.6 times (36.1-129.0 μM), respectively. This compound also dose-dependently inhibited the Cl- conductance induced by GABA (40 μM) in the range of 1-100 μM. In addition, (+)-Bicuculline inhibited the agonistic effects of GABA (40 μM) on the α1β2γ2L receptor, functioning as an antagonist of the α1β2γ2L GABAA receptor. This action caused a parallel shift in the concentration-effect curve of GABA without affecting its maximum response. Furthermore, (+)-Bicuculline also exhibited inhibitory effects on Ca2+-activated potassium channels.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bicuculline, (+)-Bicuculline, AHP, alkaloid, d-Bicuculline, convulsant, competitive, inhibit, neurotransmitter, Inhibitor, GABAR, GABA Receptor, GABAReceptor, Gamma-aminobutyric acid Receptor, potassium, γ-Aminobutyric acid Receptor

Compound Identifiers

PubChem CID

10237