(+)-Bicuculline
GABAA receptor antagonist; blocks Ca2+-activated potassium (SK) channels. Water soluble derivative of (+)-bicuculline
| 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. |
| Cell experiment [1]: | |
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Cell lines |
Primary cortical neurons from rat E18 embryos |
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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. |
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Reacting condition |
10 μM for 15–60 min |
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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]: | |
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Animal models |
13-month old Fischer- 344 virgin female ovariectomized rats. |
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Dosage form |
3.5 mg/kg( dissolved in sesame oil + 10% DMSO) daily by injection for 26 days |
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Application |
The GABAA antagonist bicuculline attenuated progesterone-induced memory impairments in middle-aged ovariectomized rats. |
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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. |
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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. |
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| Description | (+)-Bicuculline is a classical antagonist of GABAa. | |||||
| Targets | GABAa | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
