| Name | Bicuculline |
| Description | Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors, originally identified in 1932 from plant alkaloid extracts, and isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and various Corydalis species. |
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 16.67 mg/mL (45.37 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | GABA Receptor | convulsant | inhibit | alkaloid | potassium | γ-Aminobutyric acid Receptor | AHP | Bicuculline | Gamma-aminobutyric acid Receptor | competitive | Inhibitor | neurotransmitter |
| Inhibitors Related | Valproic acid sodium salt | DL-Menthol | p-Hydroxybenzaldehyde | Penicillin G sodium salt | Valproic Acid | Halothane | Chlorothymol | Piperazine citrate | Riluzole | Gabapentin | (-)-α-Pinene | Methionine |
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