| Bioactivity | 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[1]. |
| Target | Ki: 0.46 nM (rat α4β2 nAChR) and 1.2 nM (human α4β2 nAChR) |
| Invitro | 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]. |
| In Vivo | Epiboxidine (20 μg/kg; ip; once) treatment shows marked analgetic activity in mice[1].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]. Animal Model: |
| Name | Epiboxidine |
| CAS | 188895-96-7 |
| Formula | C10H14N2O |
| Molar Mass | 178.23 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fitch RW, et al. Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg Med Chem. 2004;12(1):179-190. [2]. Badio B, et al. Synthesis and nicotinic activity of epiboxidine: an isoxazole analogue of epibatidine. Eur J Pharmacol. 1997;321(2):189-194. |