212332-35-9
中文名称
4-(5-ETHOXY-3-PYRIDINYL)-N-METHYL-(3E)-3-BUTEN-1-AMINE DIFUMARATE
英文名称
4-(5-ETHOXY-3-PYRIDINYL)-N-METHYL-(3E)-3-BUTEN-1-AMINE DIFUMARATE
CAS
212332-35-9
分子式
C20H26N2O9
MOL 文件
212332-35-9.mol
212332-35-9 结构式
基本信息
中文别名
化合物 T23425化合物 TC 2559 DIFUMARATE
英文别名
TC 2559 (fumarate)TC 2559 DIFUMARATE
4-(5-ETHOXY-3-PYRIDINYL)-N-METHYL-(3E)-3-BUTEN-1-AMINE DIFUMARATE
物理化学性质
熔点123-125°C
储存条件Desiccate at RT
溶解度DMSO (Slightly), Methanol (Slightly)
形态Solid
颜色White to Off-White
水溶解性Soluble to 100 mM in water
常见问题列表
生物活性
TC-2559 difumarate 是 CNS 选择性，具有口服活性的烟碱乙酰胆碱受体 (nAChR) α4β2 亚型的部分激动剂。TC-2559 difumarate 对 α2β4、α4β4 和 α3β4 受体表现出选择性，EC50在 10-30 µM 范围内。体内研究
TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice.
TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats.
| Animal Model: | Adult male mice (body weight 15-30 g) (formalin test) |
| Dosage: | 1, 3, 10 mg/kg |
| Administration: | I.p. |
| Result: | Dose dependently reduced both early and late phases of formalin induced nociceptive behavioral responses. |
| Animal Model: | Adult male SD rats (body weight 200-220 g) (chronic constriction injury (CCI)) |
| Dosage: | 0.3, 1, 3 mg/kg |
| Administration: | I.p. |
| Result: | Significantly reversed CCI induced the paw withdrawal threshold decreases. |