Epiboxidine
Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
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- CAS 番号: 188895-96-7
- 分子式: C10H14N2O
- 分子量:178.23
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
Ki: 0.46 nM (rat α4β2 nAChR) and 1.2 nM (human α4β2 nAChR)[1]
体外実験
Epiboxidine has affinity and functional at central neuronal α4β2 receptors, with Kis of 0.46 and 1.2 in rat and humen[1].
Epiboxidine has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a Ki of 19[1].
Epiboxidine is much less toxic than Epibatidine[1].
Epiboxidine stimulates sodium-22 influx in PC12 and TE671 cells, with EC50s of 0.18 and 2.6 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Epiboxidine (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay[2].
Epiboxidine inhibits [3H]nicotine binding in rat cerebral cortical membranes, with a Ki of 0.6 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male NIH Swiss strain mice (25-30 g)[2]
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Dosage:50 and 100 mg/kg
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Administration:I.p.; once
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Result:Caused a dose-related Straub tail, hypomotility, hypoventilation and piloerection.
化学情報
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CAS 番号 188895-96-7
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分子量 178.23
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分子式 C10H14N2O
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SMILES
CC1=NOC([C@@H]2[C@@H]3N[C@@H](CC3)C2)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Fitch RW, et al. Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg Med Chem. 2004;12(1):179-190. [Content Brief]
[2]. Badio B, et al. Synthesis and nicotinic activity of epiboxidine: an isoxazole analogue of epibatidine. Eur J Pharmacol. 1997;321(2):189-194. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Epiboxidine 関連分類
HY-138953 関連分類
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