Epiboxidine hydrochloride 

Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with K_is 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].

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 K_i 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，K_i 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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，K_i 为 0.6 nM^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

214.69

C₁₀H₁₅ClN₂O

862909-67-9

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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]