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Cat. No. M2347
(+)-Bicuculline Structure


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100mg USD 100 In stock
250mg USD 220 In stock
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Quality Control
Biological Activity

(+)-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 Experiment
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.
Concentrations 10 μM
Incubation time 15-60 min
Animal Experiment
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 367.35
Formula C20H17NO6
CAS Number 485-49-4
Purity 99.81%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C

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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Keywords: (+)-Bicuculline, d-Bicuculline supplier, GABA Receptor, inhibitors

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