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.
For research use only. We do not sell to patients.
- CAS No.: 862909-67-9
- Formula: C10H15ClN2O
- Molecular Weight:214.69
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 862909-67-9
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Appearance Solid
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Molecular Weight 214.69
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)