| Description | Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species. |
| In vivo | (+)-Bicuculline（1/3 μM）使γ-氨基丁酸的EC50值分别提高1.6 倍 (41.0-67.0 μM) 和3.6 倍(36.1-129.0 μM)。(+)-Bicuculline（1-100 μM）剂量依赖性的抑制γ-氨基丁酸（40 μM）产生的Cl-电导。(+)-Bicuculline也使γ-氨基丁酸（40 μM）对α1β2γ2L受体的激动作用受到抑制。 (+)-Bicuculline是α1β2γ2LGABAA受体的拮抗剂,可使γ-氨基丁酸浓度-效应曲线发生平行移动,但不影响γ-氨基丁酸的最大反应。此外,(+)-Bicuculine对Ca2+激活的钾离子通道也有抑制作用。 |
| Target activity | GABAA receptor:2 μM |
| Synonyms | 荷包牡丹碱, (+)-Bicuculline, d-Bicuculline |
| molecular weight | 367.35 |
| Molecular formula | C20H17NO6 |
| CAS | 485-49-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 16.67 mg/mL (45.37 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Huang SH, et al. Eur J Pharmacol, 2003, 464(1), 1-8. 2. Khawaled R, et al. Pflugers Arch, 1999, 438(3), 314-321. |