| Bioactivity | Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) [1][2][3]. |
| Target | IC50: 2 μM (GABAA) |
| Invitro | Bicuculline ((+)-Bicuculline; d-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 α1β2γ2L GABAA receptors[3]. |
| Name | Bicuculline |
| CAS | 485-49-4 |
| Formula | C20H17NO6 |
| Molar Mass | 367.35 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. Br J Pharmacol. 2013;169(2):328-336. [2]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999;438(3):314-321. [3]. Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464(1):1-8. |