epibatidine

Epibatidine 2HCl is a potent nicotinic agonist.

Epibatidine是α7nACh的激动剂，Kd值为100 nM。Epibatidine可用于阿尔茨海默病、帕金森病和精神分裂症的研究。

Hemicholinium 3 是一种竞争性的、高亲和力的胆碱转运蛋白 (HACU) 抑制剂，Ki=25 nM。它是一种神经肌肉阻滞剂，能够抑制乙酰胆碱 (ACh)的合成和释放。它抑制Epibatidine 诱发的收缩和 [3H] 乙酰胆碱释放，IC50分别为 897 nM 和 693 nM。

Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

Epiboxidine 是一种有效的选择性神经nAChR 激动剂，对大鼠和人α4β2nAChR 的Ki 分别为 0.46 nM 和 1.2 nM。Epiboxidine 是生物碱 Epibatidine 的甲基异恶唑类似物，也是另一种烟碱样受体激动剂 ABT 418 的类似物。

Epiboxidine hydrochloride 是一种有效的选择性神经nAChR 激动剂，对大鼠和人α4β2nAChR 的Ki 分别为 0.46 nM 和 1.2 nM。Epiboxidine hydrochloride 是生物碱 Epibatidine 的甲基异恶唑类似物，也是另一种烟碱样受体激动剂 ABT 418 的类似物。