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Natural Products
(+)-Bicuculline

(+)-Bicuculline

Catalog No.

N1592

GABAA receptor antagonist,competitve and classical

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Grouped product items
Size	Price	Stock	Qty
10mM (in 1mL DMSO)	$116.00	In stock
100mg	$110.00	In stock
250mg	$220.00	In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

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

Product Citation

1. Jing Wang, Yue Gao, et al. "Increased NMDARs in neurons and glutamine synthetase in astrocytes underlying autistic-like behaviors of Gabrb1−/− mice." iScience. 2023 Jul 25;26(8):107476. PMID: 37599823

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	367.11
Cas No.	485-49-4
Formula	C₂₀H₁₇NO₆
Synonyms	Bucuculline
Solubility	insoluble in EtOH; insoluble in H2O; ≥13.1 mg/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
SDF	Download SDF
Canonical SMILES	CN([C@@H]1[C@H]2C(C=CC3=C4OCO3)=C4C(O2)=O)CCC(C1=C5)=CC6=C5OCO6
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

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

Quality Control

Quality Control & MSDS

View current batch:

Purity = 99.10%

Chemical structure

(+)-Bicuculline