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编 号:F236273
分子式:C10H14N2O
分子量:178.23
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生物活性:
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.

体内研究:
Epiboxidine (20 μg/kg; ip; once) treatment shows marked analgetic activity in mice.Epiboxidine (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay.Epiboxidine inhibits [3H]nicotine binding in rat cerebral cortical membranes, with a Ki of 0.6 nM.Animal Model:Adult male NIH Swiss strain mice (25-30 g)
Dosage:50 and 100 mg/kg
Administration:I.p.; once
Result:Caused a dose-related Straub tail, hypomotility, hypoventilation and piloerection.

体外研究:
Epiboxidine has affinity and functional at central neuronal α4β2 receptors, with Kis of 0.46 and 1.2 in rat and humen.Epiboxidine has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a Ki of 19.Epiboxidine is much less toxic than Epibatidine.Epiboxidine stimulates sodium-22 influx in PC12 and TE671 cells, with EC50s of 0.18 and 2.6 μM.
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