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(+)-Bicuculline

In stock
Catalog No.
N1592
GABAA receptor antagonist,competitve and classical
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
100mg
$100.00
In stock
250mg
$200.00
In stock

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Background

GABAA receptor antagonist; blocks Ca2+-activated potassium (SK) channels. Water soluble derivative of (+)-bicuculline

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt367.11
Cas No.485-49-4
FormulaC20H17NO6
SynonymsBucuculline
Solubility≥13.1mg/mL in DMSO
Chemical Name(6R)-6-[(5S)-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-6H-furo[3,4-g][1,3]benzodioxol-8-one
SDFDownload SDF
Canonical SMILESCN1CCC2=CC3=C(C=C2C1C4C5=C(C6=C(C=C5)OCO6)C(=O)O4)OCO3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Primary cortical neurons from rat E18 embryos

Preparation method

The solubility of this compound in DMSO >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM for 15–60 min

Applications

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.

Animal experiment [2]:

Animal models

13-month old Fischer- 344 virgin female ovariectomized rats.

Dosage form

3.5 mg/kg( dissolved in sesame oil + 10% DMSO) daily by injection for 26 days

Application

The GABAA antagonist bicuculline attenuated progesterone-induced memory impairments in middle-aged ovariectomized rats.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Xu J1, Kurup P1, et al, Synaptic NMDA Receptor Activation Induces Ubiquitination and Degradation of STEP61. Mol Neurobiol. 2017 May 2. doi: 10.1007/s12035-017-0555-x.

[2] Braden BB1, Kingston ML, et al, The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats. Front Aging Neurosci. 2015 Aug 14;7:149. doi: 10.3389/fnagi.2015.00149. eCollection 2015.

Biological Activity

Description (+)-Bicuculline is a classical antagonist of GABAa.
Targets GABAa          
IC50            

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