(+)-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.
|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.|
|Incubation time||15-60 min|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO: ≥ 40 mg/mL|
The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats.
Braden BB, et al. Front Aging Neurosci. 2015 Aug 14;7:149. PMID: 26321945.
Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors.
Huang SH, et al. Eur J Pharmacol. 2003 Mar 7;464(1):1-8. PMID: 12600688.
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