862909-67-9

862909-67-9 structure
862909-67-9 structure
  • Name: Epiboxidine hydrochloride
  • Chemical Name: Epiboxidine hydrochloride
  • CAS Number: 862909-67-9
  • Molecular Formula: C10H15ClN2O
  • Molecular Weight: 214.69
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
  • Create Date: 2023-06-20 14:11:31
  • Modify Date: 2024-01-10 16:05:55
  • 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[1].

Name Epiboxidine hydrochloride
Description 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[1].
Related Catalog
In Vitro Epiboxidine hydrochloride 对中枢神经元 α4β2 受体具有亲和力和功能性,在大鼠和人体内的 Ki 分别为 0.46 和 1.2[1]。 Epiboxidine hydrochloride 对 PC12 细胞神经节型 α3β4*-烟碱样受体具有活性,Ki 为 19[1]。 Epiboxidine hydrochloride 的毒性远低于 Epibatidine[1]。 Epiboxidine hydrochloride 刺激 PC12 和 TE671 细胞中的 sodium-22 内流,EC50s 分别为 0.18 和 2.6 μM[2]。
In Vivo Epiboxidine hydrochloride(20 μg/kg;腹腔注射;一次)治疗在小鼠体内显示出显着的镇痛活性[1]。 Epiboxidine hydrochloride(50 和 100 mg/kg;腹膜内注射;一次)在热板试验中引起显着的抗伤害作用[2]。 Epiboxidine hydrochloride 抑制 [3H]尼古丁在大鼠大脑皮层膜中的结合,Ki 为 0.6 nM[2]。
References

[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.  

Molecular Formula C10H15ClN2O
Molecular Weight 214.69