Epiboxidine hydrochloride
Epiboxidine hydrochloride 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 hydrochloride 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: 862909-67-9
- 分子式: C10H15ClN2O
- 分子量:214.69
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
Epiboxidine hydrochloride has affinity and functional at central neuronal α4β2 receptors, with Kis of 0.46 and 1.2 in rat and humen[1].
Epiboxidine hydrochloride has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a Ki of 19[1].
Epiboxidine hydrochloride is much less toxic than Epibatidine[1].
Epiboxidine hydrochloride 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.
Epiboxidine hydrochloride (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay[2].
Epiboxidine hydrochloride 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.
化学情報
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CAS 番号 862909-67-9
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性状 Solid
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分子量 214.69
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分子式 C10H15ClN2O
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Color White to off-white
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SMILES
CC1=NOC([C@@H]2[C@@H]3N[C@@H](CC3)C2)=C1.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
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 hydrochloride 関連分類
HY-138953A 関連分類
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