Epiboxidine hydrochloride

Names

[ Name ]:
Epiboxidine hydrochloride

Biological Activity

[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]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₀H₁₅ClN₂O

[ Molecular Weight ]:
214.69

Related Compounds

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