156223-05-1
中文名称
(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3'-联吡啶二盐酸盐
英文名称
3-(2,4-dimethoxybenzylidene)anabaseine
CAS
156223-05-1
分子式
C19H22Cl2N2O2
MOL 文件
156223-05-1.mol
更新日期
2024/07/14 19:18:32
156223-05-1 结构式
基本信息
中文别名
GTS-21盐酸盐GTS-21二盐酸盐
(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3'-联吡啶二盐酸盐
英文别名
DMXBDMXB-A
GTS-21HCl
GTS 21 2HCl
GTS-21 (DMXB-A)
DMBX-anabaseine
GTS 21 2HCl(DMXBA)
GTS21
GTS 21
GTS-21
GTS 21 2hydrochloride
GTS 21 dihydrochloride
所属类别
生物化工：激动剂抑制剂物理化学性质
熔点216-217℃ (decomposition)
储存条件2-8°C
溶解度在水中的溶解度>5mg/mL
形态粉末
颜色淡黄色至深黄色
InChIKeyRPYWXZCFYPVCNQ-RVDMUPIBSA-N
常见问题列表
生物活性
GTS-21 dihydrochloride 是一种选择性 α7 烟碱乙酰胆碱受体 (α7-nAChR) 激动剂，具有抗炎和增强认知的活性。GTS-21 dihydrochloride 也是 α4β2 (human α4β2: Ki=20 nM) 和 5-HT3A 受体 (IC50=3.1 μM) 拮抗剂。靶点
|
α7-nAChR
|
human α4β2 20 nM (Ki) |
5-HT 3A Receptor 3.1 μM (IC 50 ) |
体外研究
GTS-21 bound to human α4β2 nAChR (K i =20 nM) 100-fold more potently than to humanα7-nAChR, and is 18- and 2-fold less potent than (-)-nicotine at human α4β2 and a7 nAChR, respectively.
体内研究
GTS 21 (4 mg/kg; i.p.; 1, 3, 7, 14 and 21 days) reduces radiation induced histological signs of pulmonary injury.
| Animal Model: | C57BL6 mice were irradiated with 12 Gy to induce a mouse model of Radiation induced lung injury (RILI) |
| Dosage: | 4 mg/kg |
| Administration: | I.p.; 1, 3, 7, 14 and 21 days |
| Result: | Reduces lung inflammatory infiltrate and fibrosis in radiation treated mice. |