| 货号 | 2736/10 |
| 别名 | 6-[5-[(2S)-2-Azetidinylmethoxy]-3-p |
| 供应商 | Tocris |
| 生物活性 | Subtype-selectiveα4β2 nicotinic acetylcholine receptor ligand (Ki values are 0.26 and 54 nM at α4β2 and α3β4 receptors respectively). May act as a silent desensitizer or as an agonist, depending on subunit stoichiometry (EC50 = 1.1 nM for nAChR-stimulated dopamine release). Exhibits analgesic activity in vivo and significantly reduces nicotine self-administration in an experimental rat model. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 333.25 |
| 分子式 | C15H22Cl2N2O2 |
| 可溶性/溶解性 | Soluble to 50 mM in water |
| CAS号 | 820231-95-6 |
| 参考文献 | Levinet al (2010) Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J.Pharmacol.Exp.Ther. 332 933. PMID: 20007754. Cucchiaroet al (2008) Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 109 512. PMID: 18719450. Zwartet al (2008) Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol. 731843. Xiaoet al (2006) Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 70 1454. PMID: 16857741. |