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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- No. CAS: 188895-96-7
- Fòrmula: C10H14N2O
- Peso molecular:178.23
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
Ki: 0.46 nM (rat α4β2 nAChR) and 1.2 nM (human α4β2 nAChR)[1]
In Vitro
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.
In Vivo
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.
Chemical Information
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No. CAS 188895-96-7
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Peso molecular 178.23
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Fòrmula C10H14N2O
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SMILES
CC1=NOC([C@@H]2[C@@H]3N[C@@H](CC3)C2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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)
Epiboxidine Related Classifications
HY-138953 Related Classifications
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