(+)-Bicuculline (Synonyms: NSC 32192) |
| Catalog No.GN10745 |
(+)-Bicucline ((+)-Bicucline )) is a competitive GABAA receptor antagonist with an IC50 of 2μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 485-49-4
Sample solution is provided at 25 µL, 10mM.
(+)-Bicucline ((+)-Bicucline )) is a competitive GABAA receptor antagonist with an IC50 of 2μM [1]. (+)-Bicuculline also inhibits Ca2+-activated potassium channels [2]. (+)-Bicuculline reduces the effects of GABA without affecting the effects of glycine [3].
In vitro, (+)-Bicuculline (10 μM) treated primary cortical neuronal cells of rat E18 embryos for 15–60 min, enhanced neuronal synaptic NMDAR signaling, down-regulated STEP 61 expression, and accompanied the STEP substrate GluN 2B , increased tyrosine phosphorylation of Pyk 2 and ERK 1/2 [4]. (+)-Bicuculline (10μM) treatment of rat hippocampal neuron cells can cause calcium oscillations [5].
In vivo, (+)-Bicuculline (3.5mg/kg) treated Ovx rats via daily subcutaneous injection significantly reversed progesterone-induced cognitive decline and alleviated working memory impairment [6]. (+)-Bicuculline (1, 2, 4 mg/kg) affects the auditory steady-state response (ASSR) of SD rats through subcutaneous injection, dose-dependently reduces the ASSR signal, and significantly decreases within 10-30 minutes after administration Spectral Perturbation (ERSP) [7].
References:
[1]Collins M , Duke R , Huang S ,et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors.[J].European Journal of Pharmacology, 2003, 464(1):1-8.
[2]Khawaled R , Bruening-Wright A , Adelman J P ,et al.Bicuculline block of small-conductance calcium-activated potassium channels[J].Pflügers Archiv, 1999, 438(3):314-321.
[3]Johnston G A. Advantages of an antagonist: bicuculline and other GABA antagonists[J].British Journal of Pharmacology, 2013.
[4]Xu J1, Kurup P1, et al. Synaptic NMDA Receptor Activation Induces Ubiquitination and Degradation of STEP61 [J]. Mol Neurobiol. 2017.
[5]Maiorov S A, Kairat B K, Gaidin S G, et al. Activation of the Cannabinoid Receptors Suppresses Hyperexcitation of Rat Hippocampal Neuronal Networks In Vitro[J]. Biochemistry (Moscow), Supplement Series A: Membrane and Cell Biology, 2023, 17(2): 169-175.
[6]Blair B B , Kingston M L , Koenig E N ,et al. The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats[J].Frontiers in Aging Neuroscience, 2015.
[7]Yamazaki M, Honda S, Tamaki K, et al. Effects of (+)-bicuculline, a GABAa receptor antagonist, on auditory steady state response in free-moving rats[J]. PLoS One, 2020, 15(7): e0236363.
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Cell experiment [1]: |
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Cell lines |
Primary cortical neurons |
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Preparation method |
Primary cortical neurons were isolated from rat E18 embryos. Cells were plated on poly-D-lysine-coated plates(1×106 cells/well) in Neurobasal Media supplemented with 2% B27 and grown for 14–18 days. Neurons were treated with (+)-Bicuculline (10μM for 15–60min), picrotoxin (50μM for 15–60 min), or D-serine(100μM for 30–120 min). |
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Reaction Conditions |
10μM ; 15–60min |
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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. |
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Animal experiment [2]: |
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Animal models |
13-month old Fischer-344 virgin female rats |
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Preparation method |
rats ovaries and the tips of uterine horns were ligatured and removed. Beginning two days after surgery all drugs were administered via two daily subcutaneous injections in the scruff of the neck. For the first injection, animals received either a control vehicle solution or progesterone. For the second injection, animals received either a control vehicle solution or (+)-Bicuculline (3.5 mg/kg; dissolved in sesame oil + 10% DMSO). |
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Dosage form |
3.5 mg/kg; s.c. |
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Applications |
The GABAA antagonist (+)-Bicuculline attenuated progesterone-induced memory impairments in middle-aged ovariectomized rats. |
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References: [1]Xu J1, Kurup P1, et al. Synaptic NMDA Receptor Activation Induces Ubiquitination and Degradation of STEP61 [J]. Mol Neurobiol. 2017. [2]Blair B B , Kingston M L , Koenig E N ,et al. The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats[J].Frontiers in Aging Neuroscience, 2015. |
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| Cas No. | 485-49-4 | SDF | |
| Synonyms | NSC 32192 | ||
| 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 | ||
| Canonical SMILES | CN1CCC2=CC3=C(C=C2C1C4C5=C(C6=C(C=C5)OCO6)C(=O)O4)OCO3 | ||
| Formula | C20H17NO6 | M.Wt | 367.11 |
| Solubility | ≥ 13.1mg/mL in DMSO | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.724 mL | 13.6199 mL | 27.2398 mL |
| 5 mM | 0.5448 mL | 2.724 mL | 5.448 mL |
| 10 mM | 0.2724 mL | 1.362 mL | 2.724 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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- Purity: >99.00%
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