Bicuculline methiodide
Based on 5 publication(s) in Google Scholar
Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
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- 純度: 99.93%
- CAS 番号: 40709-69-1
- 分子式: C21H20INO6
- 分子量:509.29
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Bicuculline methiodide
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生物活性
Bicuculline methiodide (30 μM) promotes N-methyl-d-aspartate (NMDA) stimulation to facilitate burst firing in dopamine neurons[1].
Cluster discharges in the lateral habenular nucleus (LHb) of the antireward center are sufficient conditions for depression to occur. LHb neurons are usually classified into three types: silent, tonic-firing, burst-firing[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
(-)-Bicuculline methobromide (0.6 nmol/rat) attenuates the antiallodynic effect of Neurotropin[3].
(-)-Bicuculline methobromide can be used in animal modeling to create epilepsy models and is capable of crossing the blood-brain barrier[4].
Administration: 12.5, 25, 50 or 100 ng/0.25 μL • inject into SN or corpus striatum through bilateral catheter implantation
(2) Simultaneously administer bilateral infusions at a rate of 0.25 μ L/min, and after the infusion is completed, insert the catheter in situ for an additional minute to prevent drug reflux.
(3) Due to the short-lived effect of (-) - Bicuculine methoromide in SN, rats were tested 5 minutes after completing the infusion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 40709-69-1
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性状 Solid
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分子量 509.29
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分子式 C21H20INO6
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Color White to off-white
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SMILES
C[N+]1([C@](C2=C(CC1)C=C3C(OCO3)=C2)([H])[C@@]4([H])C5=C(C6=C(OCO6)C=C5)C(O4)=O)C.[I-]
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別名
(+)-Bicuculline methiodide; d-Bicuculline methiodide; (-)-ビククリンメチオジド
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Novelty exploration-activated ensemble in the lateral hypothalamus confers analgesic and anxiolytic effects. [Abstract]2026 May 19;17(1):4418. PMID: 42156381 -
Cell Rep
Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]2025 May 14;44(5):115712. PMID: 40372911 -
Brain Behav Immun
Trans-cinnamaldehyde improves neuroinflammation-mediated NMDA receptor dysfunction and memory deficits through blocking NF-κB pathway in presenilin1/2 conditional double knockout mice. [Abstract]2019 Nov:82:45-62. PMID: 31376499 -
Neurosci Bull
FOXG1 Hierarchically Shapes Synaptic Functions in Striatal iSPNs and Contributes to ASD Etiology. [Abstract]2026 Feb 2. PMID: 41627775 -
溶剤 & 溶解度
DMSO : 150 mg/mL (294.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (49.09 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.64 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Johnson SW, et al. Bicuculline methiodide potentiates NMDA-dependent burst firing in rat dopamine neurons by blocking apamin-sensitive Ca2+-activated K+ currents. Neurosci Lett. 1997 Aug 1;231(1):13-6. [Content Brief]
[2]. Yang Y, et al. Ketamine blocks bursting in the lateral habenula to rapidly relieve depression[J]. Nature, 2018, 554(7692): 317-322. [Content Brief]
[3]. Okazaki R, et al. The antiallodynic effect of Neurotropin is mediated via activation of descending pain inhibitory systems in rats with spinal nerve ligation. Anesth Analg. 2008 Sep;107(3):1064-9. [Content Brief]
[4]. Sperber EF, et al. Nigral infusions of muscimol or bicuculline facilitate seizures in developing rats. Brain Res. 1987 Dec 15;465(1-2):243-50. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9635 mL | 9.8176 mL | 19.6352 mL | 49.0879 mL |
| 5 mM | 0.3927 mL | 1.9635 mL | 3.9270 mL | 9.8176 mL | |
| 10 mM | 0.1964 mL | 0.9818 mL | 1.9635 mL | 4.9088 mL | |
| 15 mM | 0.1309 mL | 0.6545 mL | 1.3090 mL | 3.2725 mL | |
| 20 mM | 0.0982 mL | 0.4909 mL | 0.9818 mL | 2.4544 mL | |
| 25 mM | 0.0785 mL | 0.3927 mL | 0.7854 mL | 1.9635 mL | |
| 30 mM | 0.0655 mL | 0.3273 mL | 0.6545 mL | 1.6363 mL | |
| 40 mM | 0.0491 mL | 0.2454 mL | 0.4909 mL | 1.2272 mL | |
| DMSO | 50 mM | 0.0393 mL | 0.1964 mL | 0.3927 mL | 0.9818 mL |
| 60 mM | 0.0327 mL | 0.1636 mL | 0.3273 mL | 0.8181 mL | |
| 80 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6136 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1964 mL | 0.4909 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Bicuculline methiodide 関連分類
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